CAS: 2095393-15-8; (2-Chloro-4-Phenoxyphenyl)(4-(((3R,6S)-6-(Hydroxymethyl)Tetrahydro-2H-Pyran-3-yl)Amino)-3H-Pyrrolo[2,3-D]Pyrimidin-5-yl)Methanone

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    📜2-氯-4-氟苯腈置于正丁基锂,Sodium Hydride,Potassium Carbonate,N,N-二异丙基乙胺,Potassium Hydroxide体系中,用 四氢呋喃,乙醇,正己烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 13.17H,反应生成化合物arq531
    参考文献:テトラヒドロピラニルアミノ−ピロロピリミジノンおよびその使用の方法
    标题:テトラヒドロピラニルアミノ−ピロロピリミジノンおよびその使用の方法
    摘要:提供一种强效的小分子btk抑制剂,可能用于治疗免疫障碍,癌症,心血管疾病,病毒感染,炎症,代谢/内分泌功能障碍和神经障碍.通过调节btk活性的化合物(i)或其药学上可接受的盐,异构体,前药,溶剂合物,代谢产物,多形体,类似物或衍生物的药学组合物,用于治疗或预防与btk有关的疾病.

    海关参考信息

    专利信息


    专利号:US-2024262834-A1
    优先权日:2021-05-28
    标 题:Synthesis of btk inhibitor and intermediates thereof
    发明人:CHEN YONGGANG; CORRY JAMES; DESMOND RICHARD; DI MASO MICHAEL J; FORSTATER JACOB H; KUETHE JEFFREY T; KUHL NADINE; LARSON REED; LEVESQUE FRANCOIS; NARSIMHAN KARTHIK; OTTE DOUGLAS; PRIER CHRISTOPHER K; SHEVLIN MICHAEL; SIROTA ERIC; TAN LUSHI; THAISRIVONGS DAVID A; TURNBULL BEN W H; WANG ZHIXUN; XIAO KAIJIONG
    权利人:MERCK SHARP & DOHME LLC
    摘要:The present invention relates to efficient synthetic processes useful in the preparation of Compound A, a BTK inhibitor of Formula (I): or a pharmaceutically acceptable salt thereof, including the preparation of intermediates used to make Compound A or a pharmaceutically acceptable salt thereof.

    专利号:US-12441733-B2
    优先权日:2018-03-26
    标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
    发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
    权利人:NOVARTIS AG
    摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

    专利号:AU-2022280865-A1
    优先权日:2021-05-28
    标 题 :Synthesis of btk inhibitor and intermediates thereof

    专利号:WO-2022251404-A1
    优先权日:2021-05-28
    标 题:Synthesis of btk inhibitor and intermediates thereof

    专利号:AU-2022280865-A9
    优先权日:2021-05-28
    标 题:Synthesis of btk inhibitor and intermediates thereof

    专利号:EP-4347599-A1
    优先权日:2021-05-28
    标 题:Synthesis of btk inhibitor and intermediates thereof

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Woyach JA, Stephens DM, Flinn IW, Bhat SA, Savage RE, Chai F, Eathiraj S, Reiff SD, Muhowski EM, Granlund L, Szuszkiewicz L, Wang W, Schwartz B, Ghori R, Farooqui MZH, Byrd JC. First-in-Human Study of the Reversible BTK Inhibitor Nemtabrutinib in Patients with Relapsed/Refractory Chronic Lymphocytic Leukemia and B-Cell Non-Hodgkin Lymphoma. Cancer Discov. 2024 Jan 12;14(1):66-75. doi: 10.1158/2159-8290.CD-23-0670. 15(1):166. doi: 10.1186/s13045-022-01386-1.
    3: Odetola O, Ma S. Relapsed/Refractory Chronic Lymphocytic Leukemia (CLL). Curr Hematol Malig Rep. 2023 Oct;18(5):130-143. doi: 10.1007/s11899-023-00700-z. Epub 2023 Jun 6.
    4: Rivera NR, Zewge D, Arvary R, Lin M, Lohani S. Development and validation of a GC method for a key nemtabrutinib intermediate: Implementation of an in-situ free base sample preparation protocol. J Pharm Biomed Anal. 2024 Apr 15;241:116002. doi: 10.1016/j.jpba.2024.116002. Epub 2024 Feb 1. 14(22):8247. doi: 10.3390/jcm14228247.

    合成参考文献


    参考文献:10.1182/bloodadvances.2022008121
    摘要:Lim YS, Yoo SM, Patil V, Kim HW, Kim HH, Suh B, Park JY, Jeong NR, Park CH, Ryu JH, Lee BH, Kim P, Lee SH. Orally bioavailable BTK PROTAC active against wild-type and C481 mutant BTKs in human lymphoma CDX mouse models. Blood Adv. 2023 Jan 10;7(1):92–105.
    参考文献:10.1016/j.ejmech.2023.115403
    摘要:Chen S, Chen Z, Lu L, Zhao Y, Zhou R, Xie Q, Shu Y, Lin J, Yu X, Wang Y. Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy. European Journal of Medicinal Chemistry. 2023 Jul;255():115403. doi: 10.1016/j.ejmech.2023.115403.
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