噻唑烷盐酸盐 | 14446-47-0

• 物质功能分类: 有机原料 - 杂环化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 中文名称: 噻唑烷盐酸盐
• 英文名称: thiazolidine hydrochloride
• 英文别名: 1,3-thiazolidin-3-ium;chloride
• CAS: 14446-47-0
• 化学式: C₃H₇NS*ClH
• 分子量: 125.622
• InChiKey: MPGQQQKGAXDBDN-UHFFFAOYSA-N

物化性质

• 熔点：
  180 °C(Solv: water (7732-18-5))

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  6
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  37.3
• 氢给体数：
  2
• 氢受体数：
  2

安全信息

• 危险性防范说明：
  P280,P305+P351+P338
• 危险性描述：
  H302
• 储存条件：
  室温和干燥环境

反应信息

• 作为反应物：
  描述：

  噻唑烷盐酸盐 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 反应 2.0h， 以63%的产率得到2-(methylamino)ethanethiol hydrochloride
  参考文献：
  名称：

  Reversible inactivation of bovine plasma amine oxidase by cysteamine and related analogs

  摘要：

  Cysteamine (1) was reported many years ago to reversibly inhibit lentil seedling amine oxidase, through the formation of a complex with thioacetaldehyde, the turnover product of 1. Herein, cysteamine (1) and its analogs 2-(methylamino)ethanethiol (3) and 3-aminopropanethiol (6) were found to be reversible inhibitors of bovine plasma amine oxidase (BPAO), but 2-(methylthio)ethylamine (7) was determined to be a weak irreversible inhibitor of BPAO. Based on our results, indicating the necessity of a sulfhydryl-amine for reversible inactivation of BPAO, the failure of inhibited BPAO to recover activity after gel filtration, the first-order kinetics of activity recovery upon dialysis, and 2,4,6-trihydroxyphenylalanine quinine (TPQ) cofactor transformation which indicated from the results of phenylhydrazine titration and substrate protection, we propose a mechanism for the reversible inactivation of BPAO by 1 involving the formation of a cofactor adduct, thiazolidine, between BPAO and 1. (C) 2010 Elsevier Inc. All rights reserved.

  DOI：

  10.1016/j.bbrc.2010.11.052
• 作为产物：
  描述：

  聚合甲醛 、 半胱胺盐酸盐 以 水 、 异丙醇 为溶剂， 生成 噻唑烷盐酸盐
  参考文献：
  名称：

  [EN] PROCESS FOR THE PREPARATION OF TENELIGLIPTIN AND ITS NOVEL INTERMEDIATES
  [FR] PROCÉDÉ DE PRÉPARATION DE TENELIGLIPIN ET NOUVEAUX INTERMÉDIAIRES CORRESPONDANTS

  摘要：

  本发明涉及一种用于制备替格列汀或其药用可接受盐及其水合物的新型方法。该发明还涉及用于合成替格列汀的新型中间体及其制备方法。

  公开号：

  WO2015173779A1

文献信息

• SUBSTITUTED 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRIDINE-3(2H)-ONES AND 2,5,6,7-TETRAHYDRO-3H-PYRROLO[2,1-C][1,2,4]TRIAZOL-3-ONES, AND USE THEREOF
  申请人：BAYER AKTIENGESELLSCHAFT

  公开号：US20190160048A1

  公开（公告）日：2019-05-30

  The present application relates to novel substituted 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-3(2H)-ones and 2,5,6,7-tetrahydro-3H-pyrrolo[2,1-c][1,2,4]triazol-3-ones, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of lung inflammation disorders.

  该申请涉及新颖的取代5,6,7,8-四氢[1,2,4]三唑并[4,3-a]吡啶-3(2H)-酮和2,5,6,7-四氢-3H-吡咯[2,1-c][1,2,4]三唑-3-酮，其制备方法，以及其单独或组合使用用于治疗和/或预防疾病，以及其用于生产用于治疗和/或预防疾病的药物，特别是用于治疗和/或预防肺部炎症性疾病。
• Heterocyclic compounds containing nitrogen and sulfur, pharmaceutical
  申请人：Richter Gedeon Vegyeszeti Gyar Rt.

  公开号：US05096902A1

  公开（公告）日：1992-03-17

  The invention relates to novel nitrogen- and sulfur-containing heterocyclic compounds of the formula (I), acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## Ar stands for an optionally mono- or polysubstituted aryl or heteroaryl group; R.sup.1 means a carbonyl or (C.sub.2-6 alkenyl)carbonyl group; R.sup.2 stands for hydrogen C.sub.1-6 alkyl, phenyl or phenyl (C.sub.1-4 alkyl) group; R.sup.3 means hydrogen or (C.sub.1-6 alkoxy)carbonyl group; R.sup.4 and R.sup.5 stand, independently from each other, for hydrogen or C.sub.1-6 alkyl group; R.sub.6 ogen, C.sub.1-6 alkyl group or halophenyl group; m is 0 or 1; and n is 1 or 2, with the proviso that R.sup.2 means hydrogen when m is 0. The compounds of formula (I) show a significant cerebral antihypoxic action and thus, they can be used for the treatment of diseases caused by hypoxic brain damages such as e.g. the senile dementia, Alzheimer's disease or disturbances of the cognitive function.

  该发明涉及一种新的含氮和硫杂环化合物，其化学式为（I），以及其酸盐、含有它们的药物组合物和制备它们的方法。在化学式（I）中，Ar代表可选择地单取代或多取代的芳基或杂芳基；R1表示羰基或（C2-6烯基）羰基基团；R2代表氢、C1-6烷基、苯基或苯基（C1-4烷基）基团；R3表示氢或（C1-6烷氧基）羰基基团；R4和R5独立地代表氢或C1-6烷基基团；R6 ogen、C1-6烷基基团或卤苯基团；m为0或1；n为1或2，但R2在m为0时表示氢。化合物（I）表现出显著的脑部抗缺氧作用，因此可以用于治疗由缺氧性脑损伤引起的疾病，如老年性痴呆、阿尔茨海默病或认知功能障碍。
• Thiazolidine derivatives, process for their preparation and
  申请人：Chiesi Farmaceutici S.p.A.

  公开号：US04775676A1

  公开（公告）日：1988-10-04

  Compounds of formula I ##STR1## wherein A represents: a saturated or unsaturated acyclic residue; a saturated cyclic or heterocyclic residue; a saturated or unsaturated bicyclic residue; and R represents OH, a C.sub.1 -C.sub.4 alkoxy group or a straight or heterocycle aminoresidue; R.sub.1 represents hydrogen, an alkyl group or an aromatic or heteroaromatic residue. Compounds I are endowed with valuable therapeutic characteristics.

  式I的化合物，其中A代表：饱和或不饱和的无环残基；饱和的环状或杂环残基；饱和或不饱和的双环残基；R代表OH，C.sub.1 -C.sub.4烷氧基团或直链或杂环氨基残基；R.sub.1代表氢，烷基团或芳香或杂芳香残基。化合物I具有宝贵的治疗特性。
• Thiazolidine derivatives, process for their preparation and pharmaceutical compositions
  申请人：CHIESI FARMACEUTICI S.p.A.

  公开号：EP0222371A3

  公开（公告）日：1989-11-29

  Compounds of formula I wherein A represents: - a saturated or unsaturated acyclic residue; - a saturated cyclic or heterocylic residue; - a saturated or unsaturated bicyclic residue and R represents OH, a C₁-C₄ alkoxy group or a straight or heterocycle aminoresidue; R₁ represents hydrogen, an alkyl group or an aromatic or heteroaromatic residue.Compounds I are endowed with valuable therapeutic characteristics.

  式I中的化合物，其中A代表：- 饱和或不饱和的非环状残基；- 饱和的环状或杂环残基；- 饱和或不饱和的双环残基；R代表OH、C₁-C₄烷氧基团或直链或杂环氨基残基；R₁代表氢、烷基团或芳香或杂芳香残基。化合物I具有宝贵的治疗特性。
• 一种(2S)-4-氧代-2-(3-噻唑烷基羰基)-1-吡咯烷羧酸叔丁酯的合成方法
  申请人：山东邹平大展新材料有限公司

  公开号：CN110724138B

  公开（公告）日：2022-11-22

  本发明公开了一种(2S)‑4‑氧代‑2‑(3‑噻唑烷基羰基)‑1‑吡咯烷羧酸叔丁酯的合成方法，属于化学合成的技术领域。本发明的技术方案为：以L‑羟基脯氨酸为原料，先经过Boc保护反应得到化合物II，再经过氧化反应得到化合物III，最后经过取代反应，得到化合物IV；合成化合物II和化合物III为连续反应。其中，化合物II为Boc‑L‑羟脯氨酸，化合物III为N‑Boc‑4‑氧代‑L‑脯氨酸，化合物IV为(2S)‑4‑氧代‑2‑(3‑噻唑烷基羰基)‑1‑吡咯烷羧酸叔丁酯。本发明的有益效果为：(1)化合物II和化合物III实现了连续生产，大大的简化了操作难度和设备占用，并且缩短了生产周期，最大程度减少了产品损耗，提高了收率。(2)本工艺路线收率及产品质量稳定，可以达到工业生产需求。