CAS: 1013920-15-4; (S,Z)-N-(1-(Dimethylcarbamoyl)Pyrrolidin-3-yl)-5-((5-Fluoro-2-Oxoindolin-3-Ylidene)Methyl)-2,4-Dimethyl-1H-Pyrrole-3-Carboxamide

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上下游产品

5-((Z)-(5-氟-2-氧代吲哚烷-3-亚基)甲基)-2,4-二甲基-1H-吡咯-3-羧酸 5-((Z)-(5-Fluoro-2-Oxoindolin-3-Ylidene)Methyl)-2,4-Dimethyl-1H-Pyrrole-3-Carboxylic Acid 356068-93-4

合成工艺路线路线简述

    📜5-((Z)-(5-氟-2-氧代吲哚烷-3-亚基)甲基)-2,4-二甲基-1H-吡咯-3-羧酸置于o-(1H-Benzotriazol-1-yl)-N,N,N',N'-Tetramethyluronium Hexafluorophosphate,N,N-二异丙基乙胺,三氟乙酸体系中,用 二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 16.83H,反应生成伏罗尼布
    参考文献:Vegfr抑制剂vorolanib的合成方法
    标题:Vegfr抑制剂vorolanib的合成方法
    摘要:本发明提供了vegfr抑制剂vorolanib的合成方法.Vorolanib不仅在诸如非小细胞肺癌,肾细胞癌,肝细胞癌的实体肿瘤疾病上有很好的治疗效果,而且在眼部疾病治疗药物开发上具有很好的前景.本发明从设计合成路线出发,通过数次工艺考察,包括原料,温度,缩合剂,溶剂,化学反应时间,后处理几个方面,得到相对成本低,收率高,后处理简单,绿色环保的vorolanib合成路线.

    专利信息


    专利号:US-12240808-B2
    优先权日:2021-05-28
    标 题 :Process for the synthesis of calebin-a and its intermediates
    发明人:MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; MUTHUKAMAN NAGARAJAN; NAIDU PENTAKOTA PARADESI
    权利人:MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; MUTHUKAMAN NAGARAJAN; NAIDU PENTAKOTA PARADESI
    摘要:The invention discloses novel intermediates in the synthesis of Calebin A represented by formula 3. The invention also covers processes for the synthesis of Calebin-A and its analogs using compounds of formula 3.

    专利号:US-11401273-B2
    优先权日:2018-11-20
    标题:Asymmetric synthesis of Azaspiro compounds
    发明人:LELETI RAJENDER REDDY; WAMAN YOGESH; KALLURE PRIYA; BEGUM ZUBEDA; DIVYA THUMBAN; NALIVELA KUMARA SWAMY; VIJAY SAURABH; PARIKH PARANJAY; KOTTURI SHARADSRIKAR; PATEL CHIRAG; NAYAK KRISHNA; BAHAROONI KASIMRAZA; ZALAVADIYA VINKAL
    权利人:PIRAMAL PHARMA LTD
    摘要:The present invention relates to an improved asymmetric synthesis of azaspiro or diazaspiro compound (hereafter referred to as the compound 5, (5A) or (5N)) or their pharmaceutically acceptable salts and derivatives; through the formation of intermediate compounds 4, (4A) or (4N) respectively. The process comprises an unusual substrate specific highly diastereoselective as well as enantio-enriched 1-substituted 2-azaspiro[3.3]heptane or 1-substituted 2-diazaspiro[3.3]heptane compounds with high diastereoselectivity by addition of a cyclobutane carboxylate anion to a Davis-Ellman's imine, followed by reduction and cyclisation resulting in the selective formation of azaspiro or diazaspiro intermediate compound 4, (4A) or (4N); which on subsequently removing the sulfinyl group provides corresponding azaspiro or diazaspiro compound 5, (5A) or (5N) respectively.

    专利号:US-9611255-B2
    优先权日:2015-06-10
    标题 :Process for total synthesis of flavonoid compounds and isomers thereof
    发明人:RAO BATCHU VENKATESWARA; LINGAMURTHY MACHA; RAJU Gurrapu; SARMA VANKA UMAMAHESWARA
    权利人:COUNCIL SCIENT IND RES; COUNCIL SCIENT IND RES
    摘要:The present invention relates to the a process for total synthesis of flavonoid compounds of general formula I and isomers thereof n nwherein R 1 and R 2 is OH; R 3 â•?H orn n n n n n n n n n n The present invention particularly relates to the process for preparation and separation of (2S,3S)-taxifolin-6-C-β-D-glucopyranoside (ulmoside A), (2R,3R)-taxifolin-6-C-β-D-glucopyranoside and taxifolin.

    专利号:US-5338488-A
    优先权日:1992-09-10
    标 题:Process for the production of synthesis gas by oxidative converson of methane (or natural gas) using composite catalyst containing transitional and alkine earth metal oxides
    发明人:CHOUDHARY VASANT R; RAJPUT AMARJEET M; SANSARE SUBHASH D; PRABHAKAR BATHULA; MAMMAN AJIT S
    权利人:COUNCIL OF SCIENT RESEARCH
    摘要:The invention relates to a process for the production of synthesis gas by oxidative conversion of methane using composite catalysts having the formula: TmAOn, wherein T is a transition metal or metals, m is the T/A mole ratio and is from 0.01 to 100, A is an alkaline earth metal or metals, O is oxygen and n is the number of oxygen atoms needed to form a catalyst composite wherein each element of the composite has a complete set of valence electrons. In a preferred embodiment, the process includes passing a gas containing methane and oxygen over the composite catalyst in a fixed bed reactor at a pressure in the range of 0.5-50 atm, and at a temperature in the range of 200 DEG -1000 DEG C., and recovering the synthesis gas.

    专利号:US-2024199637-A1
    优先权日:2021-04-21
    标题 :Improved process for the preparation of 7-(morpholinyl)-2-(n-piperazinyl)methylthieno[2, 3-c]pyridine derivatives
    发明人:KOMPELLA AMALA; VAGICHERLA KAMESWARA RAO; LANKI REDDY TIRUMALA REDDY; PESARU NARMADA; MUDDASANI PULLA REDDY; NANNAPANENI VENKAIAH CHOWDARY
    权利人:NATCO PHARMA LTD
    摘要:The present invention describes an improved second generation process for the synthesis of NRC-1111 (1,5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-7-(4-morpholinyl)thieno[2,3-c] pyridine-5-yl]-2-pyrimidinamine) dimethane sulfonate and NRC-1109 (II, 5-[3-methyl-2-[(4-methylsulfonylpiperazin-1-yl)methyl]-7-morpholino-thieno[2,3-c]pyridin-5-yl]pyrimidin-2-amine) dimethane sulfonate. This process is cost effective, high yielding and industrially feasible process for the synthesis of compounds of formulae I and II with high purity. Formula (I) Formula (I): Râ•?H for NRC-1111 and Formula (II): Râ•?CH3 for NRC-1109 NRC-1111 and NRC-1109 are potential anti-cancer agents.

    专利号:US-11884623-B2
    优先权日:2022-05-23
    标题:Process for the preparation of (R)-4-propyl pyrrolidine-2-one, a key intermediate for synthesis of brivaracetam
    发明人:DIVI MURALI KRISHNA PRASAD; BOLNENI NAGESWARA RAO; BANDARUPALLI LEELA MAHESWARA RAO
    权利人:DIVIS LABORATORIES LTD
    摘要:A process for the preparation of (R)-4-propyl-pyrrolidine-2-one, is provided which includes enzymatic conversion of dimethyl 3-propyl pentanedioate selectively into (S)-3-(2-methoxy-2-oxoethyl) hexanoic acid using Novozyme's Promea® enzyme, amidation of (S)-3-(2-methoxy-2-oxoethyl) hexanoic acid, followed by ester hydrolysis to obtain (S)-3-(2-amino-2-oxoethyl) hexanoic acid having high chiral purity >99% and converting the amide to amine by Hofmann rearrangement and cyclization resulting in (R)-4-propyl-pyrrolidine-2-one. It is further converted to Brivaracetam by N-alkylation with 2-bromobutyric acid, esterification followed by enzymatic resolution.

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    合成参考文献


    参考文献:10.1007/978-3-031-40901-1_14
    摘要:Thapa B, Nelson A, Kilari D. Novel Targets in Development for Advanced Renal Cell Carcinoma. 2023. In: Integrating Multidisciplinary Treatment for Advanced Renal Cell Carcinoma.
    参考文献:10.1134/s107036322315001x
    摘要:Balakin KV. Analysis of the Structural Transformations Underlying the Design of Innovative Next-in-Class Drugs. Russ J Gen Chem. 2023 Dec;93(S2):S401–25. doi: 10.1134/s107036322315001x.
    参考文献:10.1007/s40278-024-59646-9
    摘要:Multiple drugs. Reactions Weekly. 2024 May 25;2009(1):390. doi: 10.1007/s40278-024-59646-9.
    参考文献:10.1007/978-3-662-69670-5_3
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