3-(2-Chlorobenzoyl)-1,3-thiazolidine-2-thione | 900587-02-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 3-(2-Chlorobenzoyl)-1,3-thiazolidine-2-thione
• 英文别名: (2-chlorophenyl)-(2-sulfanylidene-1,3-thiazolidin-3-yl)methanone
• CAS: 900587-02-2
• 化学式: C₁₀H₈ClNOS₂
• 分子量: 257.765
• InChiKey: MCCNXPKABORMPV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  77.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-氮杂双环[1.1.0]丁烷 、 3-(2-Chlorobenzoyl)-1,3-thiazolidine-2-thione 在 magnesium triflate 作用下， 以 四氢呋喃 为溶剂， 以46%的产率得到2-[1-(2-chlprobenzoyl)azetidin-3-yl]thio-1,3-thiazoline
  参考文献：
  名称：

  Reaction of 1-Azabicyclo[1.1.0]butane with Activated Amides

  摘要：

  1-Azabicyclo[1.1.0]butane (ABB, 1) reacted with 3-acyl-1,3-thiazolidine-2-thiones (7,11a-m) in the presence of a catalytic amount of Mg(OTf)(2) to give the corresponding 2-(1-acylazetidin-3-yl)thio-1,3-thiazolines (8,12a-m). It was hypothesized that this reaction is primarily influenced by a steric bulkiness of acyl groups in 3-acyl-1,3-thiazolidine-2-thiones. Resulting compounds (8, 12k) were readily converted to thiols (13,14), and azetidine-3-thiol hydrochloride (15), which is the key intermediate of 1-(1,3-thiazolin-2-yl)azetidine-3-thiol hydrochloride (4) useful for the preparation of a new oral 1 beta-methylcarbapenem antibiotic L-084, was obtained quantitatively by hydrolysis of 14.

  DOI：

  10.3987/com-09-11677

文献信息

• NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES
  申请人：Hu Lihong

  公开号：US20100113498A1

  公开（公告）日：2010-05-06

  The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.

  该发明提供了以下式1所表示的长春碱衍生物或其生理上可接受的盐，它们的制备、用途以及包含所述衍生物的药物组合物。所述长春碱衍生物对肿瘤细胞系表现出抑制活性，可用作治疗恶性肿瘤的药物。
• US8168647B2
  申请人：——

  公开号：US8168647B2

  公开（公告）日：2012-05-01
• Reaction of 1-Azabicyclo[1.1.0]butane with Activated Amides
  作者：Kazuhiko Hayashi、Eiko Kujime、Hajime Katayama、Shigeki Sano、Yoshimitsu Nagao

  DOI：10.3987/com-09-11677

  日期：——

  1-Azabicyclo[1.1.0]butane (ABB, 1) reacted with 3-acyl-1,3-thiazolidine-2-thiones (7,11a-m) in the presence of a catalytic amount of Mg(OTf)(2) to give the corresponding 2-(1-acylazetidin-3-yl)thio-1,3-thiazolines (8,12a-m). It was hypothesized that this reaction is primarily influenced by a steric bulkiness of acyl groups in 3-acyl-1,3-thiazolidine-2-thiones. Resulting compounds (8, 12k) were readily converted to thiols (13,14), and azetidine-3-thiol hydrochloride (15), which is the key intermediate of 1-(1,3-thiazolin-2-yl)azetidine-3-thiol hydrochloride (4) useful for the preparation of a new oral 1 beta-methylcarbapenem antibiotic L-084, was obtained quantitatively by hydrolysis of 14.