氨磺酰氯,(2-甲氧基乙基)- | 127953-87-1

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 氨磺酰氯,(2-甲氧基乙基)-
• 英文名称: N-(2-methoxyethyl)sulfamoyl chloride
• CAS: 127953-87-1
• 化学式: C₃H₈ClNO₃S
• 分子量: 173.62
• InChiKey: FZOOZHBELYJASR-UHFFFAOYSA-N

物化性质

• 沸点：
  249.7±42.0 °C(Predicted)
• 密度：
  1.381±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  9
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  63.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  cis-3-t-Butoxycarbonylamino-2-hydroxymethyl-4-oxoazetidine 、 氨磺酰氯,(2-甲氧基乙基)- 在 三乙胺 作用下， 以 乙腈 为溶剂， 反应 1.0h， 以77%的产率得到{(2S,3S)-2-[(2-Methoxy-ethyl)sulfamoyloxymethyl]-4-oxo-azetidin-3-yl}-carbamic acid tert-butyl ester
  参考文献：
  名称：

  A new class of cis-monobactam derivatives bearing a sulfamoyloxymethyl or an N-alkylsulfamoyloxymethyl group at position 4: Synthesis and antibacterial activity

  摘要：

  A new series of monobactam derivatives, bearing unsubstituted or N-monosubstituted sulfamoyloxymethyl groups in position 4 was synthesized either in racemic or in optically active form. Their in vitro antibacterial activity was tested in comparison with carumonam la and its methoxyimino derivative 1b. (C) 1998 Elsevier Science S.A. All rights reserved.

  DOI：

  10.1016/s0014-827x(98)00004-4
• 作为产物：
  描述：

  2-甲氧基乙胺 生成 氨磺酰氯,(2-甲氧基乙基)-
  参考文献：
  名称：

  Non-imidazole benzodiazepine inhibitors of farnesyl protein transferase

  摘要：

  抑制法尼基转移酶，这是一种参与ras癌基因表达的酶，可以通过具有上述公式化合物、它们的对映异构体、非对映异构体以及药物可接受的盐、前药和溶剂化物来实现。

  公开号：

  US06458783B1

文献信息

• 一类IDO抑制剂及其应用
  申请人：上海华汇拓医药科技有限公司

  公开号：CN109897011A

  公开（公告）日：2019-06-18

  本发明实施例提供了通式(I)的化合物或其药学上可接受的盐、立体异构体、互变异构形式、多晶型物、溶剂合物、前药、代谢物或同位素衍生物，其中取代基R1、R2、R0的定义如说明书所记载；本发明所合成的小分子IDO抑制剂药效作用显著，安全性高，将有希望成为一类新型的抗肿瘤药物。
• [EN] NOVEL COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS<br/>[FR] NOUVEAUX COMPOSÉS UTILISÉS COMME INHIBITEURS DE L'INDOLÉAMINE 2,3-DIOXYGÉNASE
  申请人：MERCK SHARP & DOHME

  公开号：WO2017106062A1

  公开（公告）日：2017-06-22

  Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme:(I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

  本文披露了以下公式（I）的化合物，这些化合物是IDO酶的抑制剂：（I）。本文还披露了这些化合物在潜在治疗或预防IDO相关疾病或紊乱中的用途。本文还披露了包含这些化合物的组合物。本文还披露了这些组合物在潜在治疗或预防IDO相关疾病或紊乱中的用途。
• The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors
  作者：Toshihiro Aoki、Ikumi Hyohdoh、Noriyuki Furuichi、Sawako Ozawa、Fumio Watanabe、Masayuki Matsushita、Masahiro Sakaitani、Kazutomo Ori、Kenji Takanashi、Naoki Harada、Yasushi Tomii、Mitsuyasu Tabo、Kiyoshi Yoshinari、Yuko Aoki、Nobuo Shimma、Hitoshi Iikura

  DOI：10.1016/j.bmcl.2013.10.001

  日期：2013.12

  Introducing a sulfamide moiety to our coumarin derivatives afforded enhanced Raf/MEK inhibitory activity concomitantly with an acceptable PK profile. Novel sulfamide 17 showed potent HCT116 cell growth inhibition (IC50 = 8 nM) and good PK profile (bioavailability of 51% in mouse), resulting in high in vivo antitumor efficacy in the HCT116 xenograft (ED50 = 4.8 mg/kg). We confirmed the sulfamide moiety showed no negative impact on tests run on the compound to evaluate DMPK (PK profiles in three animal species, CYP inhibition and CYP induction) and the safety profile (hERG and AMES tests). Sulfamide 17 had favorable properties that warranted further preclinical assessment (C) 2013 Elsevier Ltd. All rights reserved.
• Potent and selective, sulfamide-based human β3-adrenergic receptor agonists
  作者：Robert L. Dow、Ernest S. Paight、Steven R. Schneider、John R. Hadcock、Diane M. Hargrove、Kelly A. Martin、Tristan S. Maurer、Nancy A. Nardone、David A. Tess、Paul DaSilva-Jardine

  DOI：10.1016/j.bmcl.2004.03.089

  日期：2004.6

  A series of sulfamide-based analogs related to L-796568 were prepared and evaluated for their biological activity at the human beta(3)-adrenergic receptor (AR). This modification allows for a significant reduction in molecular weight, while maintaining single-digit nanomolar potencies at the beta(3)-AR and high selectivities versus the beta(1)- or beta(2)-AR. (C) 2004 Elsevier Ltd. All rights reserved.
• KR20230003296A
  申请人：——

  公开号：——

  公开（公告）日：——