Epaldeudomide

 

Epaldeudomide

CAS 1918159-31-5

MF C25H252HFN3O5, MW 468.5 g/mol

(3S)-3-deuterio-3-[7-[[2-fluoro-4-(morpholin-4-ylmethyl)phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione

(3S)-3-[4-[[2-Fluoro-4-(4-morpholinylmethyl)phenyl]methoxy]-1,3-dihydro-1-oxo-2H-isoindol-2-yl]-2,6-piperidinedione-3-d

KPG-818, KPG 818, ANTINEOPLASTIC, KV0TBL8MUS

Epaldeudomide (also known as KPG-818) is an investigational, next-generation immunomodulatory drug and "molecular glue" developed by Kangpu Biopharmaceuticals. Designed as a targeted therapy, it works by binding to the CRL4-CRBN E3 ubiquitin ligase complex to degrade specific proteins, showing promise in treating blood cancers, solid tumors, and autoimmune diseases.

Mechanism of Action

• Molecular Glue: It is a small molecule that acts as a modulator of the cereblon (CRBN) E3 ligase.
• Protein Degradation: It targets and induces the rapid degradation of two Ikaros zinc-finger transcription factors: IKZF3 (Aiolos) and IKZF1 (Ikaros).
• Immunomodulation: By degrading these targets, epaldeudomide triggers broad-spectrum immune responses, reduces tumor proliferation, and suppresses inflammation (such as the production of TNF-\(\alpha \)).

Therapeutic Pipeline and Research

Epaldeudomide is currently undergoing clinical evaluation to assess its safety, tolerability, and efficacy.

• Hematology/Oncology: It is being studied for the treatment of hematologic malignancies (such as multiple myeloma and lymphomas). It demonstrates potent anti-tumor and anti-angiogenic activity without several severe side effects typically associated with earlier immunomodulatory drugs.
• Autoimmune and Inflammatory Disorders: Because of its broad anti-inflammatory effects and ability to inhibit TNF-\(\alpha \), it is being explored for use against autoimmune conditions and inflammatory arthritis.

• OriginatorKangpu Biopharmaceuticals
• ClassAnti-inflammatories; Antineoplastics; Small molecules
• Mechanism of ActionCRBN protein modulators; Ubiquitin protein ligase complex modulators
• Phase IIInflammatory bowel diseases
• Phase I/IISystemic lupus erythematosus
• Phase IHaematological malignancies
• PreclinicalBehcet's syndrome; Crohn's disease; Multiple myeloma
• 06 Dec 2025Efficacy, pharmacokinetics and adverse events data from a phase I trial in Haematological malignancies presented at 67th American Society of Hematology Annual Meeting and Exposition (ASH-Hem-2025)
• 26 Nov 2025Epaldeudomide is still in phase I trials for Haematological malignancies (Second-line therapy or greater) in USA (PO, Capsule) (NCT04283097)
• 18 Nov 2025Efficacy and adverse events data from a phase I trial in Haematological malignancies released by Kangpu Biopharmaceuticals

SYN

US-10017492-B2
US-20170313676-A1

SYN

EP-3643709-A1
EP-3643709-B1
https://patentscope.wipo.int/search/en/detail.jsf?docId=EP293972088&_cid=P21-MPEVL7-37300-1

Example 37: Compound A382

[0196]  3-(4-((2-fluoro-5-(3-morpholinopropoxy)benzyl)amino)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, A382.

[0197]  ¹H NMR (DMSO- d ₆, 300 MHz): δ 11.00 (s, 1H), 7.32 (t, J = 7.8 Hz, 1H), 7.22 (t, J = 7.8 Hz, 1H), 7.05-7.13 (m, 2H), 6.93 (d, J = 7.5 Hz, 1H), 6.64 (d, J = 7.8 Hz, 1H), 6.28 (t, J = 6.3 Hz, 1H), 5.07-5.13 (m, 1H), 4.38 (d, J= 5.7 Hz, 2H), 4.28 (d, J= 17.4 Hz, 1H), 4.16 (d, J= 17.4 Hz, 1H), 3.54 (t, J= 4.5 Hz, 4H), 3.42 (s, 2H), 2.85-2.97 (m, 1H), 2.57-2.63 (m, 1H), 2.26-2.38 (m, 5H), 2.00-2.09 (m, 1H). LCMS: 467.2 ([M+1] ⁺).

Example 69: Compound A406

[0296]  ( S)-3-deuterium-3-(4-((2-fluoro-4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, A406.

[0297]  ¹H NMR (DMSO- d ₆, 300 MHz): δ 10.98 (s, 1H),7.47-7.55 (m, 2H), 7.31-7.38 (m, 2H), 7.16-7.20 (m, 2H), 5.24 (s, 2H), 5.06-5.12 (m, 0.04H), 4.35 (d, J = 18.0 Hz, 1H), 4.19 (d, J = 18.0 Hz, 1H), 3.55 (br, 4H), 3.47 (s, 2H), 2.82-2.94 (m, 1H), 2.48-2.57 (m, 1H), 2.33-2.42 (m, 5H), 1.91-1.96 (m, 1H). LCMS: 469.2 ([M+1] ⁺).

ADVT

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References

• Isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereofPublication Number: US-10017492-B2Priority Date: 2014-10-30Grant Date: 2018-07-10
• Isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereofPublication Number: EP-3643709-A1Priority Date: 2014-10-30
• Isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereofPublication Number: US-2017313676-A1Priority Date: 2014-10-30
• Isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereofPublication Number: EP-3643709-B1Priority Date: 2014-10-30Grant Date: 2021-10-20

/////////epaldeudomide, ANAX LABS, KPG-818, KPG 818, ANTINEOPLASTIC, KV0TBL8MUS

#epaldeudomide, #ANAX LABS, #KPG-818, #KPG 818, #ANTINEOPLASTIC, #KV0TBL8MUS

Famlasertib

 

Famlasertib

CAS 2375591-69-6

MFC26H27ClN4O MW 447.0 g/mol

4-[[4-[3-(3-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-1-piperazineethanol

2-[4-({4-[3-(3-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl}methyl)piperazin-1-yl]ethan-1-ol
serine/threonine kinase inhibitor, amyotrophic lateral sclerosis, Prosetin, WJP32276AY

Prosetin is an orally administered blocker of MAP4K under investigation for the treatment of amyotrophic lateral sclerosis.

Famlasertib (also known as Prosetin or Prostetin/12k) is a highly potent, small-molecule inhibitor targeting the mitogen-activated protein kinase kinase kinase kinase (MAP4K) family. It is an experimental drug primarily under investigation for its neuroprotective capabilities in treating neurodegenerative disorders like amyotrophic lateral sclerosis (ALS) and as an anti-invasive agent in certain cancers

• Target Pathways: MAP4K4 (HGK), MLK1, and MLK3
• Key Properties: Orally active, blood-brain barrier penetrant (CNS-penetrant)

Mechanism of Action

Famlasertib functions by blocking the activation of the MAP4K protein family, specifically demonstrating powerful inhibitory values (\(\text{IC}_{50}\)) against subfamilies like HGK (MAP4K4), MLK3, and MLK1. By inhibiting these kinases, the compound: [1]

• Reduces Endoplasmic Reticulum (ER) Stress: It helps mitigate the unfolded protein response that triggers programmed cell death in neurons affected by misfolded protein accumulation.
• Suppresses Inflammation: It blocks inflammatory pathways associated with neurodegeneration and cell damage.
• Restrains Cell Motility: In oncology contexts, it disrupts kinase signaling linked to actin cytoskeleton remodeling, preventing malignant cells from migrating.

Primary Areas of Research

1. Amyotrophic Lateral Sclerosis (ALS)

In motor neuron models of ALS, cellular stress frequently triggers neurodegeneration. Because famlasertib easily passes through the blood-brain barrier, it is capable of directly shielding motor neurons from ER-stress-mediated cell death, extending cell viability in laboratory models.

2. Oncology (Medulloblastoma)

Recent findings published on bioRxiv indicate that famlasertib acts as a "migrastatic" agent in medulloblastoma (a type of pediatric brain tumor). It suppresses the highly invasive behavior and single-cell motility of tumor cells without exhibiting developmental toxicity.

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020163594&_cid=P21-MPGALG-31359-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=US317630245&_cid=P21-MPGALG-31359-1

Preparation of 2-(4-(4-(3-(3-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzyl)piperazin-1-yl)ethan-1-ol (Compound 12k)

Following the general procedure described above, with 4-(3-(3-chlorophenyl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)benzaldehyde (10c, 418 mg, 0.86 mmol) and 1-(2-hydroxyethyl)piperazine (224 mg, 211 μL, 1.72 mmol, 2.0 eq) as the starting materials, 2-(4-(4-(3-(3-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzyl)piperazin-1-yl)ethan-1-ol (12k) was isolated as an off-white solid (139.9 mg, 36% yield over two steps). 1H NMR (400 MHz, Methanol-d ₄) δ 8.57 (d, J=2.0 Hz, 1H), 8.54 (d, J=2.0 Hz, 1H), 7.80 (s, 1H), 7.76 (d, J=8.3 Hz, 2H), 7.65 (t, J=1.9 Hz, 1H), 7.64-7.57 (m, 3H), 7.42 (t, J=7.9 Hz, 1H), 7.29 (ddd, J=8.0, 2.1, 1.0 Hz, 1H), 4.27 (s, 2H), 3.93-3.86 (m, 2H), 3.62 (s, 4H), 3.41 (s, 4H), 3.35-3.31 (m, 2H) ppm. HRMS (APCI ⁺, m/z): calcd. for C ₂₆H ₂₈N ₄₀Cl [M+H ⁺]: 447.1952, found: 447.1954.

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=US469942811&_cid=P21-MPGAUU-39605-1

ADVT

ANAX LABORATORIES

WEBSITE https://www.anaxlab.com/

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References

• Design, synthesis of new 3H-imidazo[4,5-b]pyridine derivatives and evaluation of their inhibitory properties as mixed lineage kinase 3 inhibitorsPublication Name: Bioorganic & Medicinal Chemistry LettersPublication Date: 2024-03-15PMID: 38346577DOI: 10.1016/j.bmcl.2024.129652
• The emerging role of mixed lineage kinase 3 (MLK3) and its potential as a target for neurodegenerative diseases therapiesPublication Name: European Journal of Medicinal ChemistryPublication Date: 2023-09-05PMID: 37247505DOI: 10.1016/j.ejmech.2023.115511
• Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting AgentsPublication Name: Cell Chemical BiologyPublication Date: 2019-12-19PMCID: PMC7253076PMID: 31676236DOI: 10.1016/j.chembiol.2019.10.005

PAT

• Immunophilin binding agents and uses thereofPublication Number: US-2023063768-A1Priority Date: 2019-02-07
• Immunophilin binding agents and uses thereofPublication Number: WO-2020163594-A1Priority Date: 2019-02-07
• Immunophilin-dependent inhibitors and uses thereofPublication Number: US-2022193242-A1Priority Date: 2019-02-07
• Immunophilin-dependent inhibitors and uses thereofPublication Number: WO-2020163598-A1Priority Date: 2019-02-07
• Compounds, compositions and methods for inhibiting toxic endoplasmic reticulum stress - Patents.comPublication Number: JP-7487170-B2Priority Date: 2018-03-01Grant Date: 2024-05-20
• Compounds, compositions, and methods for suppressing toxic endoplasmic reticulum stress
• Publication Number: US-2021040091-A1
• Priority Date: 2018-03-01G

///////famlasertib, serine/threonine kinase inhibitor, amyotrophic lateral sclerosis, Prosetin, WJP32276AY

#famlasertib, #serine/threonine kinase inhibitor, #amyotrophic lateral sclerosis, #Prosetin, #WJP32276AY

Fexlamose

 

Fexlamose

CAS 1285607-08-0

MFC12H22O9S2 MW374.4 g/mol

(2S,3S,4S,5R,6R)-2-(sulfanylmethyl)-6-[(2R,3R,4S,5S,6S)-3,4,5-trihydroxy-6-(sulfanylmethyl)oxan-2-yl]oxyoxane-3,4,5-triol

• 6-Thio-alpha-D-glucopyranosyl 6-thio-alpha-D-glucopyranoside
• alpha-D-Glucopyranoside, 6-thio-alpha-D-glucopyranosyl 6-thio-
• 6-thio-alpha-D-glucopyranosyl 6-thio-alpha-D-glucopyranoside; 6,6'-dithiotrehalose

6-thio-α-D-glucopyranosyl 6-thio-α-D-glucopyranoside; 6,6'-dithiotrehalose
mucolytic, AER-01, AER 01, VY9GAK6EVR, MUC-031, MUC031

Fexlamose (formerly known as AER-01) is an experimental inhaled small-molecule drug developed by Aer Therapeutics to treat muco-obstructive lung diseases like COPD (Chronic Obstructive Pulmonary Disease) and asthma. It is a thiol-modified carbohydrate designed to break down mucus plugs in the airways

How it Works

• Mechanism: Fexlamose acts as a mucolytic by cleaving the disulfide bonds in mucus, thinning the thick secretions that block airways.
• The Problem It Targets: While many respiratory drugs manage inflammation or relax airway muscles, currently no approved treatments directly tackle mucus plugs, which are a major cause of breathing difficulties in COPD.
• Delivery: It is administered as an inhalation solution (or potentially a dry powder) directly into the lungs.
• Current Clinical Status
• Fexlamose is an investigational drug and is not yet approved for public use or commercial prescription.
• Clinical Trials: It is undergoing Phase 2a clinical studies (such as the AER-01-002 trial) to evaluate its safety, tolerability, and efficacy in adults with moderate to severe COPD.
• Study Design: These trials utilize specialized CT mucus plug scoring to identify patients who are most likely to benefit from the therapy.

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2017197360&_cid=P10-MPHQBA-11926-1

Syn

US-20230172885-A1

https://patentscope.wipo.int/search/en/detail.jsf?docId=US399239351&_cid=P10-MPHQQF-20898-1

Syn

US-20230181607-A1

https://patentscope.wipo.int/search/en/detail.jsf?docId=US399582635&_cid=P10-MPHQRV-21687-1

ADVT

ANAX LABORATORIES

WEBSITE https://www.anaxlab.com/

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References

//////////fexlamose, ANAX LABS, mucolytic, AER-01, AER 01, VY9GAK6EVR, MUC-031, MUC031

#fexlamose, #ANAX LABS, #mucolytic, #AER-01, #AER 01, #VY9GAK6EVR, #MUC-031, #MUC031

Florcicaper (18F)

 

Florcicaper (18F)

CAS 855927-17-2

MF C18H3318FO2, MW 299.4544

2-[(1S,2R)-2-(5-(¹⁸F)fluorotridecyl)cyclopropyl]acetic acid

2-((1S,2R)-2-(5-(FLUORO-18F)TRIDECYL)CYCLOPROPYL)ACETIC ACID

TRANS-9(RS)-18F-FLUORO-3,4(RS,RS)-METHYLENEHEPTADECANOIC ACID

rac-{(1R,2S)-2-[(5RS)-5-(18F)fluorotridecyl]cyclopropyl}aceticacid
imaging agent, CARDIOPET, (18F FCPHA), FDG79C95XB

CardioPET is: An F-18 labeled, modified fatty acid that provides insight into regions with decreased blood flow or metabolic insufficiency in the myocardium.; CardioPET may be used to: Identify patients that will benefit from PCI or revascularization and guide intervention, Assess myocardial viability, Evaluate CAD in patients that cannot exercise.; Agent: Muscle State Imaging Agent, Type: Fatty Acid (Labeled with Fluorine 18), Condition: Coronary Artery Disease, Status: completed enrollment.;This imaging agent exploits the dietary needs of the heart as it relates to glucose and fatty acids. By introducing a radio-labeled analog to the natural fatty acids utilized as an energy source by the heart we can visualize the anatomic location and state of the muscle within the areas defined by the specific coronary artery blood flow distribution and detect problems in advance of symptoms that would lead to a stress test.

Cardiopet is under investigation in clinical trial NCT01826773 (Cardiopet as PET Imaging Agent to Assess Myocardial Perfusion and Fatty Acid Uptake in Known or Suspected CAD Subjects).

A Phase I Study in Healthy Volunteers to Evaluate the Safety of CardioPET™ in Detection of Coronary Artery Disease

CTID: NCT00413647

Phase: Phase 1

Status: Completed

Date: 2013-06-12

PATENTS

CA-2876139-A1
CN-104684546-A
CN-114736112-A
CN-115141087-A
CN-115141087-B
CN-115141125-A
CN-115141125-B
CN-115181013-A
CN-115181013-B
CN-115850224-A
CN-115850224-B
CN-115959978-A
CN-115959978-B
CN-116041169-A
CN-116199658-A
CN-116217356-A
EP-2858630-A1
EP-4133284-A1
US-10533059-B2
US-11701429-B2
US-2015361110-A1
US-2017014528-A1
US-2020199249-A1
US-2020297854-A1
US-20230314449-A1
US-20230381092-A1
US-9409927-B2
WO-2013185032-A1
WO-2022082327-A1
WO-2023085674-A1
WO-2023236978-A1
WO-2023237092-A1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2013185032&_cid=P11-MPJ5UV-89230-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2022082327&_cid=P11-MPJ5WJ-90048-1

ADVT

ANAX LABORATORIES

WEBSITE https://www.anaxlab.com/

Discovery Solutions, Supporting the chemistry needs of clients in the Medical, Analytical and Bio Sciences

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Can't Find? Let's Connect

Phone : +91 897704 2010 /  +91 9177075735, Email : info@anaxlab.com

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References

• Nanotherapeutics for drug targetingPublication Number: WO-2013185032-A1Priority Date: 2012-06-07
• Nanotherapeutics for drug targetingPublication Number: EP-2858630-A1Priority Date: 2012-06-07
• Super lewis acidic borate esters as 18F-labeled PET probesPublication Number: US-9409927-B2Priority Date: 2013-01-24Grant Date: 2016-08-09
• Super lewis acidic borate esters as 18f-labeled pet probesPublication Number: US-2015361110-A1Priority Date: 2013-01-24
• Nanotherapeutics for drug targetingPublication Number: CA-2876139-A1Priority Date: 2012-06-07
• Nanotherapeutics for drug targetingPublication Number: US-2020297854-A1Priority Date: 2012-06-07
• Nanotherapeutics for drug targetingPublication Number: CN-104684546-APriority Date: 2012-06-07
• Diagnosis of stage b2 dmvdPublication Number: US-2023314449-A1Priority Date: 2020-04-07
• Targeted drug delivery through affinity based linkersPublication Number: US-2017014528-A1Priority Date: 2014-03-12
• Targeted drug delivery through affinity based linkersPublication Number: US-2020199249-A1Priority Date: 2014-03-12
• Targeted drug delivery through affinity based linkersPublication Number: US-10533059-B2Priority Date: 2014-03-12Grant Date: 2020-01-14
• Targeted drug delivery through affinity based linkersPublication Number: US-11701429-B2Priority Date: 2014-03-12Grant Date: 2023-07-18

//////////florcicaper (18F), anax labs, imaging agent, CARDIOPET, (18F FCPHA), FDG79C95XB

#florcicaper (18F), #anax labs, #imaging agent, #CARDIOPET, #(18F FCPHA), #FDG79C95XB

Florensocatib

 

Florensocatib

CAS 2762114-61-2

MF C23H23FN4O4 MW438.5 g/mol

(2S)-N-[(1S)-1-cyano-2-[2-fluoro-4-(3-methyl-2-oxo-1,3-benzoxazol-5-yl)phenyl]ethyl]-1,4-oxazepane-2-carboxamide

(2S)-N-{(1S)-1-cyano-2-[2-fluoro-4-(3-methyl-2-oxo-2,3-dihydro1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-
carboxamide
cathepsin inhibitor, HSK 31858, CHF 10196, DPP1-IN-1, RWC743JRK7

Florensocatib (originally designated as HSK31858 or CHF10196) is an investigative, highly potent, oral reversible inhibitor of dipeptidyl peptidase 1 (DPP1). It is being actively researched for its ability to reduce the frequency of pulmonary exacerbations in adults suffering from inflammatory respiratory diseases like bronchiectasis

Mechanism of Action

DPP1 (also known as cathepsin C) is a lysosomal protease enzyme responsible for activating neutrophil serine proteases (NSPs). In conditions like non-cystic fibrosis bronchiectasis, hyperactive neutrophils accumulate in the airways, causing severe tissue damage, chronic inflammation, and airway widening.

By inhibiting DPP1, florensocatib prevents the activation of these damaging enzymes, effectively targeting the primary driver of neutrophilic inflammation in the lungs.

Clinical Development & Trial Progress

Florensocatib is undergoing global evaluation across multiple advanced clinical trials:

• The SAVE-BE Trial: An earlier clinical phase where the drug demonstrated high potency and favorable efficacy profiles in treating inflammatory lung conditions.
• The HOPE-BE Trial: A definitive Phase III protocol launched to evaluate the long-term safety and overall reduction of pulmonary exacerbation frequencies specifically among Chinese adults.
• Global Phase III Status: According to records on ClinicalTrials.gov, randomised, double-blind trials are evaluating the drug against a placebo in participants aged 12 to 85 for treatment windows stretching up to 78 weeks.

SYN

US11807635,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US395653715&_cid=P21-MPKKTA-33002-1

Example 1: (S)—N—((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazepane-2-carboxamide (Compound 1)

Step 4: (S)—N—((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazepane-2-carboxamide (Compound 1)

1D (0.32 g, 0.59 mmol) was dissolved in formic acid (2.5 mL) and upon completion of the addition, the mixture was reacted at 50° C. for 10 min. The reaction solution was concentrated to dryness and ethyl acetate (20 mL) was added. Then saturated aqueous sodium bicarbonate solution was added dropwise to adjust the pH to about 8. The organic layer was separated and the remaining aqueous layer was extracted with ethyl acetate (25 mL×3). The organic phases were combined, dried over anhydrous sodium sulfate, filtered and concentrated, and the residue was separated and purified by silica gel column chromatography (dichloromethane:methanol (v/v)=20:1) to obtain the title compound 1 (0.15 g, 58.0%). LC-MS (ESI): m/z=439.1 [M+H] +.

1H NMR (400 MHz, CDCl 3) δ 7.43-7.22 (m, 5H), 7.12 (d, 1H), 5.19 (dd, 1H), 4.18-4.04 (m, 1H), 4.05-3.95 (m, 1H), 3.78 (m, 1H), 3.46 (s, 3H), 3.41-3.17 (m, 3H), 3.03-2.87 (m, 3H), 1.88 (m, 2H).

SYN

US11807635,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US395653715&_cid=P21-MPKKYT-35548-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2022042591&_cid=P21-MPKKS9-32509-1

(S)-N-((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazepane-2-carboxamide(compound 1)

Step 4: (S)-N-((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazacycloheptane-2-carboxamide (Compound 1) 

[0360]

(S)-N-((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazepane-2-carboxamide(compound 1)

[0361]1D (0.32 g, 0.59 mmol) was dissolved in formic acid (2.5 mL), and the mixture was reacted at 50 °C for 10 min after the addition was complete. The solution was concentrated to dryness, and ethyl acetate (20 mL) was added. The pH was adjusted to approximately 8 by dropwise addition of saturated sodium bicarbonate solution. The organic layer was separated and extracted with ethyl acetate (25 mL × 3). The organic phases were combined, dried over anhydrous sodium sulfate, filtered, concentrated, and the residue was purified by silica gel column chromatography (dichloromethane:methanol (v/v) = 20:1) to give title compound 1 (0.15 g, 58.0%). LC-MS (ESI): m/z = 439.1 [M+H] ⁺ . 

[0362]

¹H NMR(400MHz,CDCl ₃)δ7.43–7.22(m,5H),7.12(d,1H),5.19(dd,1H),4.18–4.04(m,1H),4.05–3.95(m,1H),3.78(m,1H),3.46(s,3H),3.41–3.17(m,3H),3.03–2.87(m,3H),1.88(m,2H).

ADVT

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References

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