CAS: 136350-52-2; 1-((4-Bromophenyl)Sulfonyl)Pyrrolidine

该化合物是一种溴化磺酰胺衍生物,其特点是与4-溴苯基混合物相连的聚氨酯-替代磺酰胺组,该化合物主要用作有机合成的中间体,特别是在研制药品和农用化学品方面,其主要优点包括:由电子退出型磺酰胺组负责的核生殖替代反应的高度反应性,以及溴代金替代体的多功能性,通过交叉组合反应进一步发挥作用.

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214210-14-7 852026-79-0 5033-22-7

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上下游产品

4-(磺酰吡咯啉)苯基硼酸 (4-(Pyrrolidin-1-Ylsulfonyl)Phenyl)Boronic Acid 486422-57-5
4-[(4-甲基哌嗪-1-基)磺酰基]苯基硼酸 4-[(4-Methylpiperazin-1-yl)Sulfonyl]Phenylboronic Acid 486422-11-1

合成工艺路线路线简述

    📜1,4-丁二醇,4-溴苯磺酰胺置于三氟甲磺酸酐体系中,用 甲苯 用作溶剂,化学反应 48.0H,以92%的收率获得1-(4-溴苯基磺酰)吡咯啉
    参考文献:N-Alkylation Of Sulfonamides With Alcohols By Tf2O
    标题:N-Alkylation Of Sulfonamides With Alcohols By Tf2O
    摘要:N-磺酰吡咯烷和n-烷基磺酰胺通过tf2O对磺酰胺与1,4-二醇或醇的烷基化反应高效合成.该反应在温和的反应条件下进行,产率中等到高,并且耐受芳香族和脂肪族磺酰胺.
    Doi:10.1246/bcsj.20150005

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    专利信息


    专利号:WO-2004020401-A1
    优先权日:2002-09-02
    标题 :Synthesis of sulfonamide derivatives
    发明人：KALLIKAT JOHN; MANDAL ASHIS BARAN; GANESH SAMBASIVAM
    权利人:SYNGENE INTERNAT PRIVATE LTD; KALLIKAT JOHN; MANDAL ASHIS BARAN; GANESH SAMBASIVAM
    摘要:The novel method of synthesis of sulphonamide derivatives (I), comprising reaction of alkyl-4-halophenylsulfonate with an amine. Formula (I) wherein X is halogen and R1 and R2 are independently selected from group comprising (i) C1 to C15 alkyl, straight or branched, (ii) C3 to C15 cycloalkyl, substituted or unsubstituted, (iii) C2 to C15 alkenyl, straight or branched, (iv) C2 to C15 alkynyl, straight or branched, (v) phenyl or benzyl, substituted or unsubstituted, (vi) heterocycloalkyl, substituted or unsubstituted, (vii) hydrogen, (viii) form with the nitrogen to which they are attached a 3-7 membered heterocyclic moiety such as pyrolidine, piperidine, piperazine, imidazole, pyrazole, (ix) the alkyl in i) may be attached to a moiety selected from cycloalkyl or heterocycloalkyl, substituted or unsubstituted

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    主要参考文献

    参考标题:Iodine-Catalyzed Sulfonylation Of Sulfonyl Hydrazides With Tert-Amines: A Green And Efficient Protocol For The Synthesis Of Sulfonamides
    作者:Jinyang Chen,Xiaoran Han,Lan Mei,Jinchuan Liu,Kui Du,Tuanwu Cao,Qiang Li
    摘要:This Study Provides A Direct, Sustainable And Eco-Friendly Method For The Synthesis Of Various Sulfonamides Via The Sulfonylation Of Sulfonyl Hydrazides With Tert-Amines. The Method Utilizes Sulfonyl Hydrazides To Oxidize And Couple With Tertiary Amines Through Selective Cleavage Of C-N Bonds. In This Reaction, Molecular Iodine Was Used As The Catalyst And T-Butyl Hydroperoxide Was Used As The Oxidant

    合成参考文献


    参考文献:10.1016/j.bbrc.2023.08.050
    摘要:Ikeda Y, Davis MI, Sumita K, Zheng Y, Kofuji S, Sasaki M, Hirota Y, Pragani R, Shen M, Boxer MB, Takeuchi K, Senda T, Simeonov A, Sasaki AT. Multimodal action of KRP203 on phosphoinositide kinases in vitro and in cells. Biochemical and Biophysical Research Communications. 2023 Oct;679():116–21. doi: 10.1016/j.bbrc.2023.08.050.
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