tert-butyl N-[4-hydroxytetrahydrofuran-3-yl]carbamate | 1430230-65-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氧唑烯
• 英文名称: tert-butyl N-[4-hydroxytetrahydrofuran-3-yl]carbamate
• 英文别名: (±)-trans-3-tert-butoxycarbonylamino-4-hydroxytetrahydrofuran；tert-butyl N-[trans-4-hydroxyoxolan-3-yl]carbamate；tert-butyl N-[(3R,4S)-4-hydroxyoxolan-3-yl]carbamate
• CAS: 1430230-65-1
• 化学式: C₉H₁₇NO₄
• 分子量: 203.238
• InChiKey: SFIADDJLFYFDGK-RNFRBKRXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  67.8
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 储存条件：
  存储条件：2-8°C，需密封并保持干燥。

反应信息

• 作为反应物：
  描述：

  tert-butyl N-[4-hydroxytetrahydrofuran-3-yl]carbamate 在 草酰氯 、 二甲基亚砜 、 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 17.0h， 以44%的产率得到tert-butyl N-(4-oxotetrahydrofuran-3-yl)carbamate
  参考文献：
  名称：

  [EN] SELECTIVE ANDROGEN RECEPTOR MODULATORS
  [FR] MODULATEURS SÉLECTIFS D'UN RÉCEPTEUR DES ANDROGÈNES

  摘要：

  本发明提供了新型选择性雄激素受体调节剂及其盐和药物组合物。

  公开号：

  WO2013055577A1
• 作为产物：
  描述：

  二碳酸二叔丁酯 、 trans-4-azido-3-hydroxytetrahydrofuran 在 palladium on activated charcoal 氢气 作用下， 生成 tert-butyl N-[4-hydroxytetrahydrofuran-3-yl]carbamate
  参考文献：
  名称：

  Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications

  摘要：

  We previously reported a series of enantiopure cis-(1 R,2S)-cyclopentyldiamine derivatives as potent and selective inhibitors of Factor Xa (FXa). Herein, we describe our approach to improve the metabolic stability of this series via core modifications. Multiple resulting series of compounds demonstrated similarly high FXa potency and improved metabolic stability in human liver microsomes compared with the cyclopentyldiamide 1. (3R,4S)-Pyrrolidinyldiamide 31 was the best overall compound with human FXa K; of 0.50 nM, PT EC2x of 2.1 mu M in human plasma, bioavailability of 25% and t z of 2.7 h in dogs. Further biochemical characterization of compound 31 is also presented. (c) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.07.020

文献信息

• SALT FORM AND CRYSTAL FORM OF COMPOUND AS FGFR4 INHIBITOR AND PREPARATION METHOD THEREOF
  申请人：GUANGDONG ZHONGSHENG PHARMACEUTICAL CO., LTD

  公开号：US20210087181A1

  公开（公告）日：2021-03-25

  The present invention provides a salt form, a crystal form, and a preparation method of a compound as an FGFR4 inhibitor and medical uses thereof.

  本发明提供了一种作为FGFR4抑制剂的化合物的盐形态、晶体形态以及制备方法，以及其医药用途。
• 4-aminobenzonitrile selective androgen receptor modulators
  申请人：Eli Lilly and Company

  公开号：US08658693B2

  公开（公告）日：2014-02-25

  The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof.

  本发明提供了新型选择性雄激素受体调节剂及其盐和制药组合物。
• Selective Androgen Receptor Modulators
  申请人：Eli Lilly and Company

  公开号：US20130217762A1

  公开（公告）日：2013-08-22

  The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof.

  本发明提供了新型选择性雄激素受体调节剂及其盐和制药组合物。
• NOVEL MORPHOLINE DERIVATIVE OR SALT THEREOF
  申请人：FUJIFILM Corporation

  公开号：US20160168139A1

  公开（公告）日：2016-06-16

  There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof. (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z 2 represents CH or the like; Z 1 represents CR 6 or the like; R 6 represents a hydrogen atom or the like; X 1 represents CHR 7 or the like; R 7 represents a hydrogen atom or the like; X 2 represents CH 2 or the like; R 1 and R 2 are the same as or different from each other, and each of R 1 and R 2 represents a hydrogen atom or the like; R 3 , R 4 , and R 5 are the same as or different from each other, and each of R 3 , R 4 , and R 5 represents a hydrogen atom, NR a R b , or the like; and each of R a and R b represents a hydrogen atom, a C 1-8 alkyl group which may have a substituent, or the like.)

  提供了一种由通式[1A]表示的吗啡啉衍生物或其盐。（在公式中，环A表示由通式[I]表示的环；*表示键合位置；Z2表示CH或类似物；Z1表示CR6或类似物；R6表示氢原子或类似物；X1表示CHR7或类似物；R7表示氢原子或类似物；X2表示CH2或类似物；R1和R2相同或不同，每个R1和R2表示氢原子或类似物；R3、R4和R5相同或不同，每个R3、R4和R5表示氢原子、NRaRb或类似物；每个Ra和Rb表示氢原子、可能具有取代基的C1-8烷基或类似物。）
• Enzymatic preparation of cis and trans-3-amino-4-hydroxytetrahydrofurans and cis-3-amino-4-hydroxypyrrolidines
  作者：Ángela Villar-Barro、Vicente Gotor、Rosario Brieva

  DOI：10.1016/j.bmc.2014.05.014

  日期：2014.10

  The lipase catalyzed resolution of cis and trans-3-amino-4-hydroxytetrahydraurans and cis-3-amino-4-hydroxypyrrolidines have been studied. For all the heterocycles, the best enantioselectivity was obtained using Candida antarctica lipases A and B as catalysts in hydrolytic processes. The absolute configuration of the optically pure obtained heterocycles has been assigned. (C) 2014 Elsevier Ltd. All rights reserved.