CAS: 444-27-9; Thiazolidine-4-Carboxylic Acid

该化合物是一种环状七环有机化合物,其特点是五人环状,含有硫和氮原子;该化合物的特点是一个箱状酸功能组,该组具有酸性,通常是在水和极有机溶剂中溶解的白色至白晶状固体,反映其极分功能组;二亚佐利丁环的存在具有独特的再活动性,使其对各种化学合成和生物应用感兴趣;四硫氨碘甲酸可参与典型的箱式酸反应,如酯化和恐吓,还可能由于硫原子的存在而进行核循环替代;其衍生物已经研究过潜在的危害性活动,包括抗微生物学和抗炎特性;总体而言,该化合物是有机合成和药用化学中有价值的建筑块.

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欧盟法规

ECHA物质C&L通报REACH预注册

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CAS号50-00-0 甲醛 | CAS号921-01-7 D-半胱氨酸 | CAS号52-89-1 L-半胱氨酸盐酸盐(无水物) | CAS号34592-47-7 L-硫代脯氨酸 | CAS号50703-06-5 噻唑烷-2-甲酸甲酯盐酸盐 | CAS号51077-16-8 N-B°C-(R)-噻唑-4-羧酸 | CAS号5025-82-1 半叶素 | CAS号1156496-63-7 4-carboxy-1,3-t... | CAS号88381-44-6 外消旋 N-亚硝基噻唑烷-4-羧酸 | CAS号640-61-9 N-甲基对甲苯磺酰胺 | CAS号34592-47-7 L-硫代脯氨酸 | CAS号63091-82-7 B°C-d-噻唑烷-4-羧酸 | CAS号66223-38-9 ethyl thiazolid... | CAS号89860-78-6 3-(2,4-dinitrop...

合成工艺路线路线简述

    L-硫代脯氨酸置于水杨醛,溶剂黄146体系中,化学反应生成 噻莫西酸
    参考文献:(Rs)-1,3-噻氮烷-4-羧酸不对称转化制备光学活性高半胱氨酸和高半胱氨酸
    标题:(Rs)-1,3-噻氮烷-4-羧酸不对称转化制备光学活性高半胱氨酸和高半胱氨酸
    摘要:来自 (Rs)-高半胱氨酸硫内酯盐酸盐 [(Rs)-Htl.hcl] 的 Dl-高半胱氨酸 [dl-Hcy] 在乙酸中与甲醛反应得到 (Rs)-1,3-噻氮烷-4-羧酸一水合物 [(Rs)-Tha.h2O].(Rs)-Tha.h2O 的不对称转化是通过在乙酸中的水杨醛存在下与旋光酒石酸形成盐来实现的.分别由 (R)-Tha 与 (2R,3R)-酒石酸的盐得到的 (R)-和 (S)-Tha 及其对映体盐用盐酸羟胺处理得到 D-和 L-Hcy分别为 100% 光学纯度,(Rs)-Htl.hcl 的产率为 50%.d-和 L-Hcy 用过氧化氢氧化分别得到 D-和 L-高胱氨酸,产率为 47%.
    DOI:10.1246/bcsj.66.536

    海关参考信息

    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-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:WO-2024165450-A1
    优先权日:2023-02-09
    标题:Method of chemical synthesis of single-chain antibody fragments and products thereby obtained
    发明人:FIGINI MARIANGELA; LUISON ELENA
    权利人:GLYTECH INC; FIGINI MARIANGELA
    摘要:A new method is disclosed for the protein full-chemical synthesis of single-chain antibody fragments (scFv); the obtained products are structurally close and functionally equivalent to their biological counterpart, being however, advantageously free of impurities and more reproducible in properties. The method includes the general steps of: (a) separately synthetizing sub-sequences (peptide fragments) (b) sequentially assembling the sub-sequences obtained in step (a) in the order as they appear in the target scFv amino acid sequence, and (c) performing oxidative folding of the assembled whole peptide molecule obtained in step (b) and dialyzing the resulting product in a buffer.

    专利号:US-8404804-B2
    优先权日:2007-08-28
    标 题 :Methods and intermediates for chemical synthesis of polypeptides and proteins
    发明人:DONG ZHENG XIN; EYNON JOHN S
    权利人:DONG ZHENG XIN; EYNON JOHN S; IPSEN PHARMA SAS
    摘要:The present invention relates to methods and intermediates for chemical synthesis of polypeptides and proteins, and more particularly to methods and intermediates for chemically ligating a peptide fragment containing N-terminal N-methyl-cysteine (SEQ ID NO: 1) with another peptide fragment having C-terminal thioester to generate a β-(methylamino)-thioester intermediate that spontaneously rearranges to form an amide bond. Furthermore, the invention relates to methods of converting N-methyl-thiazolidine to N-methyl-cysteine (SEQ ID NO: 1) of polypeptides and proteins. The invention also relates to methods of synthesizing peptide-thioester from peptide-acid fluoride.

    专利号:US-10087221-B2
    优先权日:2013-03-21
    标题 :Synthesis of hydantoin containing peptide products
    发明人:HENKEL BERND
    权利人:SANOFI AVENTIS DEUTSCHLAND
    摘要:The present invention relates to a method of synthesizing a peptide product comprising at least one hydantoin group. The peptide product may be used as a reference material for the quality control of pharmaceutical peptides, particularly for the quality control of exendin peptides. Further, the invention relates to hydantoin building blocks, a method for manufacturing such building blocks and their use for the synthesis of peptide products.

    专利号:US-9549995-B2
    优先权日:2012-03-26
    标 题:Efficient synthesis of ethylenedicysteine-sugar conjugates for imaging and therapy
    发明人:YANG DAVID J; YU DONG-FANG
    权利人:UNIV TEXAS
    摘要:Novel methods of synthesis of ethylenedicysteine-sugar conjugates and therapeutic and diagnostic applications of such conjugates are disclosed. Methods of synthesizing these conjugates in high purity are also presented as using starting materials such as thiazolidine carboxylic acid. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these conjugates prepared herein, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
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    主要参考文献

    1. Bakry RS, Razak OA, el Walily AF, Belal SF. Spectrophotometric investigation of the formed chelate between timonacic and palladium(II) and its analytical applications. J Pharm Biomed Anal. 1998 May;17(1):95-101. doi: 10.1016/s0731-7085(97)00172-6.

    合成参考文献


    摘要:Raghunathan, R.; Purushothaman, S., Science of Synthesis: Multicomponent Reactions, (2013) 2, 236.
    摘要:Lancet., 1(778), 1981
    摘要:Drugs under Experimental and Clinical Research., 13(399), 1987 []
    摘要:Lancet., 1(68), 1980 []
    摘要:R.B. Woodward, A. Neuberger and N.R. Trenner, in "The Chemistry of Penicillin", ed. H.T. Clarke, J.R. Johnson and R. Robinson, Princeton Univ. Press, Princeton, 1949, p. 415.
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