CAS: 36724-68-2; (S)-1-(2,2,2-Trifluoroacetyl)Pyrrolidine-2-Carbonyl Chloride

该化合物是有机合成和制药应用中使用的多用途三氟甲基化构件,其关键优点包括存在反应式氯乙烯组和三氟乙基苯,能够以更高的亲脂性和代谢稳定性有效地衍生出阳性碘片,三氟甲基组改进了电益性,便利了核生殖替代反应.这种化合物在浸泡性微生物和生物活性分子设计中特别有用,其结构特征有助于改善结合性和药用植物特性.由于对水分的敏感性,通常在水分条件下处理,确保合成转化中的最佳再活动.

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CAS号147-85-3 脯氨酸 | CAS号97522-31-1 (2S)-2-Benzylpy...

合成工艺路线路线简述

    📜(S)-1-(Trifluoroacetyl)Pyrrolidine-2-Carboxylic Acid置于草酰氯,N,N-二甲基甲酰胺体系中,用 二氯甲烷 用作溶剂,化学反应 3.0H,反应生成(S)-(-)-N-(三氟乙酰基)吡咯烷-2-羰酰氯
    参考文献:分子内催化生成的金属类胡萝卜素反应生成的铵化铵的重排.第2部分.双环胺的立体选择性合成
    标题:分子内催化生成的金属类胡萝卜素反应生成的铵化铵的重排.第2部分.双环胺的立体选择性合成
    摘要:由束缚在环状烯丙基胺上的铜类胡萝卜素的分子内反应产生的铵化铵经过[2,3]重排以传递双环胺.该反应可以使用其中重氮基团与氮相邻地连接的环状n-烯丙胺或其中重氮基团为n的乙烯基取代的环状胺来进行.-拴在戒指上.在前一类反应中,立体选择性叶立德的形成和重排通常可实现高水平的非对映控制.在后一种情况下,当使用对映体纯的底物进行反应时,可以实现有效的"手性转移".该反应已用于构建吡咯烷,吲哚并咪唑和喹唑烷系统,并在甘露糖胺和兽用生物碱中发现了ce亚基.
    Doi:10.1039/b108182A

    海关参考信息

    专利信息


    专利号:US-4000197-A
    优先权日:1973-07-23
    标 题 :Asymmetric synthesis of phenylisopropylamines
    发明人:BARFKNECHT CHARLES F; NICHOLS DAVID E
    权利人:UNIV IOWA RES FOUND
    摘要:The synthesis of enantiomers of a series of methoxy- and alkyl- substituted phenylisopropylamines is described. The synthesis comprises reducing the imines, formed by the reaction of appropriate phenylacetones with either (+)- or (-)-α-methylbenzylamine, by low-pressure reduction techniques, and subsequently subjecting the optically active N-(α-phenethyl)phenylisopropylamine derivative to hydrogenolysis. The hydrogenolysis products are characterized by enantiomeric purities in the range of 96 - 99%. Yields of products are approximately 60%.

    专利号:US-5468876-A
    优先权日:1986-05-22
    标题:Intermediates for the stereoconservative synthesis of 1-substituted (S)-and (R)-2-aminomethylpyrrolidines
    发明人:FEDERSEL HANS-JUEGEN; HOE THOMAS; RAEMSBY STEN I; STROEM PETER H E
    权利人:ASTRA AB
    摘要:Disclosed are (R)- and (S)-isomers of the compounds of the Formulas II and III with at least 95% optical purity ##STR1## wherein R 1 and R 2 are the same or different and represent a hydrogen atom, a lower alkyl, lower alkenyl or lower alkynyl group, a cycloalkyl group or a group (CH 2 ) m Ph, wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group. n These compounds are intermediates in the stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines.

    专利号:US-3943142-A
    优先权日:1969-01-24
    标 题:Dye intermediates and their preparation and use in the synthesis of methine dyes
    发明人:OWEN JOHN R
    权利人:EASTMAN KODAK CO
    摘要:Compositions of matter are provided comprising a stable, non-vaporous monomeric methylene base selected from a 2-methylenethiazoline; a 2-methylenebenzothiazoline; a 2-methylenenaphthothiazoline; a 2-methylenebenzoselenazoline; and a 2-methylenenaphthoselenazoline. The compositions of the invention are prepared by reacting the parent 2-methyl quaternary salt with a non-hydroxylic base which removes a proton of the heterocyclic salt together with a proton acceptor which inhibits build-up of the hydro salt of the non-hydroxylic base, the reaction being conducted under anhydrous conditions in a non-hydroxylic liquid in which the heterocyclic quaternary salt is sufficiently insoluble to inhibit dimer formation. The compositions of the invention are employed in the preparation of methine dyes.

    专利号:WO-8707271-A1
    优先权日:1986-05-22
    标 题 :A stereoconservative synthesis of 1-substituted (s)- and (r)-2-aminomethylpyrrolidines and intermediates thereto

    专利号:US-5300660-A
    优先权日:1986-05-22
    标 题:Efficient stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines and intermediates thereto

    专利号:EP-0270596-A1
    优先权日:1986-05-22
    标题 :A stereoconservative synthesis of 1-substituted (s)- and (r)-2-aminomethylpyrrolidines and intermediates thereto

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    ✅ COA系统入驻 | 共享模式

    主要参考文献

    参考标题:Palladium-Catalyzed Anti-Markovnikov Oxidation Of Allylic Amides To Protected β-Amino Aldehydes
    作者:Jia Jia Dong,Emma C. Harvey,Martín Fañanás-Mastral,Wesley R. Browne,Ben L. Feringa |发布日期:2014.12.10
    摘要:Directly From Protected Allylic Alcohols Via Palladium-Catalyzed Autotandem Reactions, And The Application Of This Method To The Synthesis Of β-Peptide Aldehydes Is Described. From A Mechanistic Perspective, We Demonstrate That Tbuoh Acts As A Nucleophile In The Reaction And That The Initially Formed Tert-Butyl Ether Undergoes Spontaneous Loss Of Isobutene To Yield The Aldehyde Product. Furthermore, Tbuoh

    合成参考文献


    参考文献:10.1007/s00216-007-1271-6
    摘要:Kraemer T, Paul LD. Bioanalytical procedures for determination of drugs of abuse in blood. Analytical and Bioanalytical Chemistry. 2007 Apr 28;388(7):1415–35. doi: 10.1007/s00216-007-1271-6.
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