CAS: 2097002-61-2; (3Ar,10R)-5-Fluoro-1,2,3,3A,8,9,10,11-Octahydro-10-Methyl-12H-15,17-Ethenopyrazolo[3,4-D]Pyrido[2,3-K]Pyrrolo[2,1-M][1,3,7]Triazacyclotridecin-12-One

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上下游产品

Ethyl 5-[(2R)-2-(2-Chloro-5-Fluoro-3-Pyridyl)Pyrrolidin-1-Yl]Pyrazolo[1,5-A]Pyrimidine-3-Carboxylate 1260847-48-0
Ethyl (R)-5-(2-(5-Fluoro-2-Methoxypyridin-3-yl)Pyrrolidin-1-yl)Pyrazolo[1,5-A]Pyrimidine-3-Carboxylate 1260845-79-1
Ethyl (R)-5-(2-(5-Fluoro-2-Oxo-1,2-Dihydropyridin-3-yl)Pyrrolidin-1-yl)Pyrazolo[1,5-A]Pyrimidine-3-Carboxylate 1260846-14-7

合成工艺路线路线简述

    📜5-氯吡唑并[1,5-A]嘧啶-3-羧酸乙酯置于盐酸,4-二甲氨基吡啶,Copper(L) Iodide,Palladium On Activated Charcoal,水,氢气,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,三乙胺,二异丙胺,Sodium Hydroxide体系中,用 1,4-二氧六环,甲醇,乙醇,二氯甲烷,异丙醇,甲苯 用作溶剂,15.0~75.0 °C,344.75 Kpa 条件下,反应 22.0H,反应生成赛利替尼
    参考文献: Formulations Of A Macrocyclic Trk Kinase Inhibitor[fr] Formulations D'Un Inhibiteur De Kinase Trk Macrocyclique
    标题: Formulations Of A Macrocyclic Trk Kinase Inhibitor[fr] Formulations D'Un Inhibiteur De Kinase Trk Macrocyclique
    摘要:本申请在某些实施例中提供了一种包括化合物(1)和混合剂的药物组合物.此外,还提供了制备药物组合物的方法和使用药物组合物的方法,例如用于治疗癌症.

    海关参考信息

    专利信息


    专利号:WO-2011148392-A1
    优先权日:2010-05-28
    标题 :Process for the preparation of (2s,4s,5s,7s)-n-(2-carbamyl-2- methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3- methoxypropoxy)phenyl]-octanamide hemifumarate and its intermediates thereof
    发明人:SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; VENKAT REDDY GHOJALA; RAMA SUBBA REDDY KARAMALA; SAHADEVA REDDY MARAMREDDY
    权利人:MSN LAB LTD; SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; VENKAT REDDY GHOJALA; RAMA SUBBA REDDY KARAMALA; SAHADEVA REDDY MARAMREDDY
    摘要:The present invention relates to a process for the preparation of (2S,4S,5S,7S)-N-(2- Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxy propoxy )phenyl]-octanamide compound of formula- 1 and its pharmaceutically acceptable salts thereof. Further, relates to the processes for the preparation of (R)-4-(2-(halomethyl)-3- methylbutyl)-l-methoxy-2-(3-methoxypropoxy) benzene and (R)-2-(4-methoxy-3-(3-methoxy propoxy) benzyl)-3-methyIbutan-l-ol useful intermediates in the synthesis of compound of formula- 1.

    专利号:US-3717556-A
    优先权日:1969-06-14
    标 题 :PROCESS FOR THE PREPARATION OF beta -HALOGENO-ALKYL-ISOCYANATES
    发明人:KAMPE K
    权利人:HOECHST AG
    摘要:N-halogeno-alkyl- Beta -lactams are rearranged into Beta halogeno-alkyl-isocyanates by contacting them with unsaturated organic compounds, optionally under irradiation. The products are highly reactive and useful for the synthesis of heterocyclic compounds.

    专利号:US-5411927-A
    优先权日:1992-08-14
    标 题 :Process of preparing composite catalysts for production of synthesis gas by oxidative conversion of methane or natural gas
    发明人:CHOUDHARY VASANT R; RANE VILAS H; RAJPUT AMARJEET M R
    权利人:COUNCIL SCIENT IND RES
    摘要:An improved process for the production of synthesis gas (or carbon monoxide and hydrogen) by oxidative conversion of natural gas or methane, which comprises passing continuously a gaseous reactant mixture comprising methane (or natural gas) and oxygen (or air) with or without water vapors over reduced or unreduced composite catalyst, containing non-transition and/or transition metal oxides, represented by the formula Tm.Nn.R.Op, wherein T is selected from Ni, CO, Ir or the like or a mixture thereof, m is T/R mole ratio, N is a transition or non-transition element selected from Ti, Zr, Hf, Zn, Mg, Ca or the like or a mixture thereof, n represents the N/R mole ratio, R is a rare earth element selected from La, Ce, Pr, Ho, Yb or the like, or a mixture thereof, O is oxygen and p is the number of oxygen atoms required to fulfill the valence requirement of the elements in the composite catalyst. Synthesis gas can be produced in high yields and with very high production rate by oxidative conversion of methane or natural gas to CO and H2 or synthesis gas, using the composite catalyst containing non-transition and/or transition metal oxides.

    专利号:EP-4217339-A1
    优先权日:2020-09-26
    标题:A process for the synthesis of anthranilic acid/amide compounds and intermediates thereof

    专利号:US-9174924-B2
    优先权日:2007-09-17
    标 题 :Hydrolysable linkers and cross-linkers for absorbable polymers
    发明人:BEZWADA RAO S
    权利人:BEZWADA BIOMEDICAL LLC
    摘要:The present invention relates to the discovery of new class of linear and multiarmed hydrolysable linkers and cross linkers for use in the synthesis of biodegradable polymers such as, polyesters, polyurethanes, polyamides, polyureas and degradable epoxy amine resin. The linear and multiarmed hydrolysable linkers of the present invention include symmetrical and/or unsymmetrical ether carboxylic acids, amines, amide diols, amine polyols and isocyanates.

    专利号:DE-2324441-A1
    优先权日:1972-05-15
    标题 :METHOD OF SYNTHESIS OF HYDROGENATION CATALYSTS

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    📌 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: Mahajan AT, Shivani, Datusalia AK, Coluccini C, Coghi P, Chaudhary S. Pyrazolo[1,5-a]pyrimidine as a Prominent Framework for Tropomyosin Receptor Kinase (Trk) Inhibitors-Synthetic Strategies and SAR Insights. Molecules. 2024 Jul 29;29(15):3560. doi: 10.3390/molecules29153560.
    2: Qin Q, Lu S, Guo Z, Li Z, Fu Q, Wang X, Wu T, Sun Y, Liu N, Zhang H, Zhao D, Cheng M. Discovery of novel indazole derivatives as second-generation TRK inhibitors. Eur J Med Chem. 2024 Oct 5;276:116640. doi: 10.1016/j.ejmech.2024.116640. Epub 2024 Jul 1. 13(12):e7393. doi: 10.1002/cam4.7393.
    4: Roa P, Foglizzo V, Harada G, Repetto M, Kulick A, de Stanchina E, de Marchena M, Auwardt S, Sayed Ahmed S, Bremer NV, Yang SR, Feng Y, Zhou C, Kong N, Liang R, Xu H, Zhang B, Bardelli A, Toska E, Ventura A, Drilon A, Cocco E. Zurletrectinib is a next-generation TRK inhibitor with strong intracranial activity against NTRK fusion-positive tumours with on-target resistance to first-generation agents. Br J Cancer. 2024 Aug;131(3):601-610. doi: 10.1038/s41416-024-02760-1. Epub 2024 Jun 20.
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