m-chlorobenzyl chloroformate | 39545-30-7

• 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: m-chlorobenzyl chloroformate
• 英文别名: 3-Chlorobenzyl carbonochloridate；(3-chlorophenyl)methyl carbonochloridate
• CAS: 39545-30-7
• 化学式: C₈H₆Cl₂O₂
• 分子量: 205.04
• InChiKey: ABNOKJAUAHDRQI-UHFFFAOYSA-N

物化性质

• 沸点：
  259.2±23.0 °C(Predicted)
• 密度：
  1.375±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  m-chlorobenzyl chloroformate 在 4-二甲氨基吡啶 、 sodium hydroxide 、 1-羟基苯并三唑 、 戴斯-马丁氧化剂 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 生成 3-[(S)-2-(3-Chloro-benzyloxycarbonylamino)-3-methyl-butyrylamino]-5-fluoro-4-oxo-pentanoic acid tert-butyl ester
  参考文献：
  名称：

  Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group

  摘要：

  This article describes the synthesis and biological evaluation of a group of N-protected Val-Asp-fmk as caspase inhibitors. The protecting group was found to contribute to caspase-3 inhibiting activity, and compounds with a large group such as Cbz are more active than compounds with a small group such as Ac. Compounds with more hydrophobic protecting groups were found to be more active in cell apoptosis protection assays, probably due to increased cell permeability. MX1122,2,4-di-Cl-Cbz-Val-Aspfmk, is identified as a potent broad-spectrum caspase inhibitor and is selective for caspases versus other proteases, with good activity in the cell apoptosis protection assays as well as good efficacy in the mouse liver apoptosis model. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.08.027
• 作为产物：
  描述：

  光气 、 3-氯苯甲醇 生成 m-chlorobenzyl chloroformate
  参考文献：
  名称：

  N,N-disubstituted aminoalkylbiphenyl antagonists of prostaglandin D2 receptors

  摘要：

  本文描述了PGD2受体拮抗剂化合物。还描述了包括这些化合物的药物组合物和药物在内的药物制剂，这些药物是PGD2受体拮抗剂。本文还描述了使用这些PGD2受体拮抗剂的方法，单独或与其他化合物结合，用于治疗呼吸系统、心血管系统和其他PGD2依赖性或PGD2介导的疾病或病症。

  公开号：

  US08362044B2

文献信息

• [EN] DIAMINOCYCLOHEXANE COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS DE DIAMINOCYCLOHEXANE ET LEURS UTILISATIONS
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2013012829A1

  公开（公告）日：2013-01-24

  The present invention provides compounds of Formula (I) or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.

  本发明提供了Formula (I)的化合物或其立体异构体，或其药学上可接受的盐，其中所有变量均如本文所定义。这些化合物是NPY Y4受体的激动剂、部分激动剂和调节剂，可用于治疗和预防各种疾病和症状。
• 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。
• [EN] CARBOXAMIDE DERIVATIVES OF PYRROLIDINE, PIPERIDINE AND HEXAHYDROAZEPINE FOR THE TREATMENT OF THROMBOSIS DISORDERS<br/>[FR] DERIVES CARBOXAMIDE DE PYRROLIDINE, PIPERIDINE ET HEXAHYDROAZEPINE UTILISES DANS LE TRAITEMENT DE TROUBLES THROMBOTIQUES
  申请人：ORTHO PHARMACEUTICAL CORPORATION

  公开号：WO1997041102A1

  公开（公告）日：1997-11-06

  (EN) Carboxamide derivatives of pyrrolidine, piperidine, and hexahydroazepine of formula (I) are disclosed as useful in treating platelet-mediated thrombotic disorders.(FR) L'invention se rapporte à des dérivés carboxamide de pyrrolidine, pipéridine et hexahydroazepine de la formule (I) qui sont utilisés dans le traitement des troubles thrombotiques induits par les plaquettes.

  （中文）公开了式（I）的吡咯烷，哌啶和六氢唑啉的羧酰胺衍生物，用于治疗血小板介导的血栓性疾病。
• N,N-disubstituted aminoalkylbiphenyl antagonists of prostaglandin D2 receptors
  申请人：Panmira Pharmaceuticals, LLC

  公开号：US08067445B2

  公开（公告）日：2011-11-29

  Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

  本文描述了一些PGD2受体拮抗剂化合物。还描述了包含这些PGD2受体拮抗剂化合物的药物组合物和药物。本文还描述了使用这些PGD2受体拮抗剂，单独或与其他化合物结合，治疗呼吸系统、心血管系统和其他依赖或介导于PGD2的疾病或病症的方法。
• N,N-DISUBSTITUTED AMINOALKYLBIPHENYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS
  申请人：HUTCHINSON John Howard

  公开号：US20120058123A1

  公开（公告）日：2012-03-08

  Described herein are compounds that are antagonists of PGD 2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD 2 receptors. Also described herein are methods of using such antagonists of PGD 2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD 2 -dependent or PGD 2 -mediated conditions or diseases.

  本文描述了一些PGD2受体拮抗剂化合物。还描述了包括这些PGD2受体拮抗剂化合物的药物组合物和药物。此外，还描述了使用这些PGD2受体拮抗剂，单独或与其他化合物联合治疗呼吸系统、心血管系统和其他PGD2依赖性或PGD2介导的疾病或病症的方法。