9H-fluoren-9-ylmethyl chlorosulfonylcarbamate | 289901-11-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: 9H-fluoren-9-ylmethyl chlorosulfonylcarbamate
• 英文别名: (9H-fluoren-9-yl)methylN-(chlorosulfonyl)carbamate；9H-fluoren-9-ylmethyl N-chlorosulfonylcarbamate
• CAS: 289901-11-7
• 化学式: C₁₅H₁₂ClNO₄S
• 分子量: 337.784
• InChiKey: BSXMXCTWIRNTJY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  80.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  9H-fluoren-9-ylmethyl chlorosulfonylcarbamate 、 在 吡啶 、 哌啶 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以22%的产率得到
  参考文献：
  名称：

  Total synthesis of malayamycin A and analogues

  摘要：

  The total synthesis of the bicyclic C-nucleoside malayamycin A is described starting with D-ribonolactone. A new method was developed to obtain preparatively important quantities of beta-pseudouridine, which was used as an intermediate. The synthesis of a carba N-nucleoside analogue of malayamycin A is also described. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2005.12.066
• 作为产物：
  描述：

  氯磺酰异氰酸酯 、 9-芴甲醇 以 甲苯 为溶剂， 生成 9H-fluoren-9-ylmethyl chlorosulfonylcarbamate
  参考文献：
  名称：

  一种氨基磺酸酯的制备方法

  摘要：

  本发明涉及一种氨基磺酸酯的制备方法。具体地，本发明公开了一种氨基磺酰化试剂，具有廉价易得、溶解度好、高稳定性等优点。使用所述试剂可高选择性地实现对羟基的氨基磺酰化修饰，反应条件温和，操作简单，可放大量。所得产物具有收率高、副产物少、纯度高等优势。

  公开号：

  CN114478373B

文献信息

• [EN] 5- (SUBSTITUTED PHENYL) -THIADIAZOLIDINE-3-ONES AND THEIR USE AS PTP1B<br/>[FR] THIADIAZOLIDINE-3-ONES 5-(PHENYLE SUBSTITUE) ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE PTP1B
  申请人：ASTRAZENECA AB

  公开号：WO2004041799A1

  公开（公告）日：2004-05-21

  The invention concerns compounds of the formula (I) or pharmaceutically acceptable salts thereof (A chemical formula should be inserted here - please see paper copy enclosed herewith) wherein R1, R2, R3, R4, R5, and R6 have any of the meanings defined in the description. Processes for the manufacture of compounds of formula (I), compositions containing them, their use as inhibitors of protein tyrosine phosphatase PTP1B and their use for the treatment of diabetes mellitus are also described.

  本发明涉及公式(I)的化合物或其药用可接受的盐（请参见随附的纸质副本中的化学公式）其中，R1、R2、R3、R4、R5和R6具有说明书中定义的任何含义。还描述了制造公式(I)化合物的方法、包含它们的组合物、它们作为蛋白酪氨酸磷酸酶PTP1B的抑制剂的使用以及它们用于治疗糖尿病的方法。
• PROCESS FOR THE SYNTHESIS OF AN INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR
  申请人：INCYTE CORPORATION

  公开号：US20150133674A1

  公开（公告）日：2015-05-14

  The present application is directed to processes and intermediates for making 4-(2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.

  本申请涉及用于制备4-(2-[(氨基磺酰)氨基]乙基}氨基)-N-(3-溴-4-氟苯基)-N′-羟基-1,2,5-噁二唑-3-羧酰胺的过程和中间体，该化合物是色胺酸2,3-二氧化酶的抑制剂，可用于治疗癌症和其他疾病。
• [EN] 1, 2, 5-THIADIAZOLIDIN-3-ONE 1, 1 DIOXIDE DERIVATIVES AS INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE PTP1B<br/>[FR] DERIVES DE 1, 2, 5-THIADIAZOLIDIN-3-ONE 1, 1 DIOXYDE UTILISES EN TANT QU'INHIBITEURS DE LA PROTEINE TYROSINE PHOSPHATASE PTP1B
  申请人：ASTRAZENECA AB

  公开号：WO2004050646A1

  公开（公告）日：2004-06-17

  The invention concerns compounds of the formula (I) or pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4, and R5 have any of the meanings defined in the description.Processes for the manufacture of compounds of formula (I), compositions containing them, their use as inhibitors of protein tyrosine phosphatase PTP1B and their use for the treatment of diabetes mellitus are also described.

  该发明涉及式(I)的化合物或其在药学上可接受的盐中，其中R1、R2、R3、R4和R5具有描述中定义的任何含义。还描述了制备式(I)化合物的方法、含有它们的组合物、它们作为蛋白酪氨酸磷酸酶PTP1B抑制剂的用途以及它们用于治疗糖尿病的用途。
• [EN] PROCESS FOR THE SYNTHESIS OF AN INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR<br/>[FR] PROCÉDÉ POUR LA SYNTHÈSE D'UN INHIBITEUR DE L'INDOLEAMINE 2,3-DIOXYGÉNASE
  申请人：INCYTE CORP

  公开号：WO2015070007A1

  公开（公告）日：2015-05-14

  The present application is directed to processes and intermediates for making 4-(2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.

  本申请涉及制备4-(2-[(氨基磺酰)氨基]乙基}氨基)-N-(3-溴-4-氟苯基)-N'-羟基-1,2,5-噁二唑-3-羧酰亚胺的工艺和中间体，该化合物是吲哚胺2,3-双加氧酶的抑制剂，可用于治疗癌症和其他疾病。
• Process for the synthesis of an indoleamine 2,3-dioxygenase inhibitor
  申请人：Incyte Corporation

  公开号：US10280157B2

  公开（公告）日：2019-05-07

  The present application is directed to processes and intermediates for making 4-(2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.

  本申请涉及制造 4-(2-[(氨基磺酰基)氨基]乙基}氨基)-N-(3-溴-4-氟苯基)-N′-羟基-1,2,5-恶二唑-3-甲脒的工艺和中间体，它是一种吲哚胺 2,3-二氧 化酶抑制剂，可用于治疗癌症和其他疾病。