噻唑烷-4-羧酸乙酯 | 66223-38-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 噻唑烷-4-羧酸乙酯
• 英文名称: ethyl L-thiazolidine-4-carboxylate hydrochloride
• 英文别名: 4-ethoxycarbonyltetrahydrothiazole hydrochloride；ethyl thiazolidine-4-carboxylate hydrochloride；Thiazolidine-4-carboxylic acid ethylester*HCl；4-ethoxycarbonylthiazolidine hydrochloride；(+/-)-(R)-thiazolidine-4-carboxylic acid ethyl ester; hydrochloride；(+/-)-(R)-Thiazolidin-4-carbonsaeure-aethylester; Hydrochlorid；Ethyl 1,3-thiazolidine-4-carboxylate hydrochloride；ethyl 1,3-thiazolidine-4-carboxylate;hydrochloride
• CAS: 66223-38-9
• 化学式: C₆H₁₁NO₂S*ClH
• mdl: MFCD00206007
• 分子量: 197.686
• InChiKey: SQRLNYSSTHJCIU-UHFFFAOYSA-N

物化性质

• 熔点：
  144-145 °C

计算性质

• 辛醇/水分配系数(LogP)：
  0.27
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.833
• 拓扑面积：
  63.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  噻唑烷-4-羧酸乙酯 在 氢溴酸 、 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 0.5h， 生成 ethyl N-(4-amino-4-methoxycarbonylbutanoyl)thiazolidine-4-carboxylate hydrobromide
  参考文献：
  名称：

  Synthesis and antitrypanosomal evaluation of some thiazole-containing amino acids and peptides

  摘要：

  Several amino acids and peptides containing thiazole and thiazolidine residues were prepared. They were tested in vivo and in vitro as possible antitrypanosomal compounds. Some derivatives showed a slight activity. As they are structurally related to glutathione, their inhibitory properties towards glutathionylspermidine synthetase, trypanothione synthetase and trypanothione reductase were determined. No inhibitory activity was found.

  DOI：

  10.1016/0223-5234(93)90125-x
• 作为产物：
  描述：

  噻莫西酸 以80%的产率得到
  参考文献：
  名称：

  HABERMEHL G. G.; ECSY W., HETEROCYCLES, 1977, 7, NO 2, 1027-1032

  摘要：

  DOI：

文献信息

• Aromatic pyrrolidine amide prolyl endopeptidase inhibitors
  申请人：Pfizer Inc

  公开号：US05847155A1

  公开（公告）日：1998-12-08

  A series of aromatic pyrrolidine derivatives and suitable pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as PEP inhibitors in the treatment of Alzheimer's disease, amnesia, dementia, anxiety ischemia, or stroke.

  本发明揭示了一系列芳香吡咯烷衍生物及其适宜的药用可接受盐。这些化合物在治疗阿尔茨海默病、健忘症、痴呆症、焦虑性缺血或中风中作为PEP抑制剂是有用的。
• 取代噻唑烷氨荒酸铋配合物及其用途
  申请人：河南全宇制药股份有限公司

  公开号：CN103992289B

  公开（公告）日：2016-04-06

  本发明公开了一种取代噻唑烷氨荒酸铋配合物及其用途，所述配合物的六种结构名称分别为：噻唑烷氨荒酸铋、2-甲基噻唑烷氨荒酸铋、2-羧基噻唑烷氨荒酸铋、2-乙氧羰基噻唑烷氨荒酸铋、S-4-羧基噻唑烷氨荒酸铋、4-乙氧羰基噻唑烷氨荒酸铋；所述配合物可用于治疗个体体内的疾病或病症，所述疾病或病症可以是癌症，包括人体结肠癌，人体乳腺癌，人体骨髓癌，人体肝癌，人体肺癌和人体白血病等；所述配合物纯度高、抗肿瘤效果好，作用菌株广谱，增加了抗肿瘤药物的种类，具有广阔的市场前景。
• 5,6,7,8 tetrahydroindolizines derivatives
  申请人：Rhona-Poulenc Rorer S.A.

  公开号：US06194426B1

  公开（公告）日：2001-02-27

  A novel therapeutic use of pyrrole derivatives of the folloeing formula: in which the variables are as defined in the specification and their salts thereof for treating conditions in which TNF is involved.

  使用以下式子中的吡咯衍生物进行新型治疗用途：其中变量如规范中定义的那样以及它们的盐，用于治疗涉及TNF的疾病。
• Phosphonoalkanoylamino acids
  申请人：ANALYTICAL RESEARCH PHARMACEUTICALS PTY. LTD.

  公开号：EP0070131A1

  公开（公告）日：1983-01-19

  Certain new phosphonoalkanoylamino acids of the formula (I) herein and their pharmaceutically acceptable salts exhibit improved antihypertensive properties and are particularly useful for the reduction of angiotensin related hypertension. in which R, and R2, which are the same or different, are each selected from the group consisting of a hydrogen atom, an optionally substituted lower alkyl, a lower alkenyl, an optionally substituted aryl and an optionally substituted aralkyl radical; n is 0 or 1; R3 is a hydrogen atom, an optionally substituted lower alkyl, a lower alkenyl, an optionally substituted aryl or an optionally substituted aralkyl group; and (a) R4 is a hydrogen atom, a lower alkyl or a phenyl-lower alkyl radical; R5 and R6, which are the same or different, are each selected from the group consisting of a hydrogen atom, an optionally substituted lower alkyl or an aryl radical; and R7 is selected from the group consisting of -OR8, -NR9 or -SR10, wherein R8 and R,o are each selected from the group consisting of a hydrogen atom, a lower alkyl, an optionally substituted aryl, or an optionally substituted aralkyl radical and Rs is a hydrogen atom, a hydroxy or lower alkyl radical or the residue of an - amino acid; or (b) R4 and R5 are part of a four-, five- or six-membered optionally substituted heterocyclic ring as a connected bridge of 2 to 4 atoms of carbon or carbon and either nitrogen, sulphur or oxygen; and R6 and R7 are each as defined in (a); with the proviso that when R3 is a hydrogen atom, n is 0, the heterocyclic ring is an unsubstituted pyrrolidine, R6 is a hydrogen atom, and R7 is ORB, at least one of R1, R2 and R8 is an optionally substituted aryl radical; or (c) R5 and R6 are selected to form a side chain of a-amino acid, where N(R4) CR5R6COR7 is an a-amino acid residue; with the proviso that (i) when R3 is hydrogen and n is 0, the a-amino acid residue is not alanine, aspartic acid, glutamic acid, glycine or phenylalanine, and (ii) when R3 is hydrogen and n is 1, the a-amino acid residue is not aspartic acid; or (d) R5 and R6 are part of a cycloalkyl ring of from 3 to 6 carbon atoms; and R4 and R7, where appropriate, are each as defined in (a); or a pharmaceutically acceptable salt of the compounds of the formula (I).

  某些新的式(I)膦酰基烷酰胺酸及其药学上可接受的盐具有更好的抗高血压特性，尤其适用于降低与血管紧张素相关的高血压。 其中相同或不同的 R 和 R2 各自选自由氢原子、任选取代的低级烷基、低级烯基、任选取代的芳基和任选取代的芳烷基组成的组； n 为 0 或 1； R3 是氢原子、任选取代的低级烷基、低级烯基、任选取代的芳基或任选取代的芳烷基；和 (a) R4 是氢原子、低级烷基或苯基-低级烷基； R5和R6（相同或不同）各自选自由氢原子、任选取代的低级烷基或芳基组成的组；以及 R7选自由-OR8、-NR9或-SR10组成的组，其中R8和R,o各自选自由氢原子、低级烷基、任选取代的芳基或任选取代的芳烷基组成的组，Rs是氢原子、羟基或低级烷基或-氨基酸的残基；或 (b) R4 和 R5 是四元、五元或六元任选取代的杂环的一部分，是 2 至 4 个碳原子或碳原子与氮、硫或氧原子的连接桥；以及 R6 和 R7 各自如(a)中定义；但当 R3 是氢原子，n 是 0，杂环是未取代的吡咯烷，R6 是氢原子，R7 是 ORB 时，R1、R2 和 R8 中至少有一个是任选取代的芳基；或 (b) R3 是氢原子，n 是 0，杂环是未取代的吡咯烷，R6 是氢原子，R7 是 ORB 时，R1、R2 和 R8 中至少有一个是任选取代的芳基。 (c) R5 和 R6 被选来形成 a-氨基酸侧链，其中 N(R4) CR5R6COR7 是 a-氨基酸残基；但(i)当 R3 为氢且 n 为 0 时，a-氨基酸残基不是丙氨酸、天冬氨酸、谷氨酸、甘氨酸或苯丙氨酸，和(ii)当 R3 为氢且 n 为 1 时，a-氨基酸残基不是天冬氨酸；或 (d) R5 和 R6 是 3 至 6 个碳原子的环烷基环的一部分；和 R4和R7（如适用）各自如(a)中定义；或式（I）化合物的药学上可接受的盐。
• Zeidler, J. M.; Emling, F.; Zimmermann, W., Archiv der Pharmazie, 1991, vol. 324, # 9, p. 687
  作者：Zeidler, J. M.、Emling, F.、Zimmermann, W.、Roth, H. J.

  DOI：——

  日期：——