1-t-butyl-3-methylazetidine-3-carbonitrile | 1353650-40-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环丁烷
• 英文名称: 1-t-butyl-3-methylazetidine-3-carbonitrile
• 英文别名: 1-(tert-Butyl)-3-methylazetidine-3-carbonitrile；1-tert-butyl-3-methylazetidine-3-carbonitrile
• CAS: 1353650-40-4
• 化学式: C₉H₁₆N₂
• 分子量: 152.239
• InChiKey: JZOHXAZONKRXQY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  27
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-t-butyl-3-methylazetidine-3-carbonitrile 在 lithium aluminium tetrahydride 、 potassium hydroxide 作用下， 以 乙醚 、 乙醇 为溶剂， 反应 123.0h， 生成 (1-Tert-butyl-3-methylazetidin-3-yl)methanol
  参考文献：
  名称：

  Synthesis of 3-functionalized 3-methylazetidines

  摘要：

  1-t-Butyl- and 1-(4-methylbenzyl)-3-bromo-3-methylazetidines were prepared from the corresponding N-(2,3-dibromo-2-methylpropylidene)alkylamines and their propensity to undergo nucleophilic substitution at the 3-position by different nucleophiles was assessed, providing a convenient access to novel 3-alkoxy-, 3-aryloxy-, 3-hydroxy-, 3-cyano-, 3-carboxy-, 3-(aminomethyl)- and 3-(hydroxymethyl)azetidines. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2011.10.097
• 作为产物：
  描述：

  3-bromo-1-t-butyl-3-methylazetidine 在 水 作用下， 生成 1-t-butyl-3-methylazetidine-3-carbonitrile
  参考文献：
  名称：

  Synthesis of 3-functionalized 3-methylazetidines

  摘要：

  1-t-Butyl- and 1-(4-methylbenzyl)-3-bromo-3-methylazetidines were prepared from the corresponding N-(2,3-dibromo-2-methylpropylidene)alkylamines and their propensity to undergo nucleophilic substitution at the 3-position by different nucleophiles was assessed, providing a convenient access to novel 3-alkoxy-, 3-aryloxy-, 3-hydroxy-, 3-cyano-, 3-carboxy-, 3-(aminomethyl)- and 3-(hydroxymethyl)azetidines. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2011.10.097

文献信息

• Fumagillol heterocyclic compounds and methods of making and using same
  申请人：Zafgen, Inc.

  公开号：US10023561B2

  公开（公告）日：2018-07-17

  Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

  本文部分公开了烟曲霉素化合物和用于治疗肥胖等疾病的方法。提供了药物组合物和制造烟嘧酚化合物的方法。这些化合物对蛋氨酰氨基肽酶 2 具有活性。
• Compounds that inhibit Mcl-1 protein
  申请人：AMGEN INC.

  公开号：US10632128B2

  公开（公告）日：2020-04-28

  Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

  本文提供了髓细胞白血病 1 蛋白（Mcl-1）抑制剂、其制备方法、相关药物组合物以及使用方法。例如，本文提供了式 I 的化合物、 或其立体异构体；以及其药学上可接受的盐类和含有这些化合物的药物组合物。本文提供的化合物和组合物可用于治疗癌症等疾病或病症。
• CARM1 INHIBITORS AND USES THEREOF
  申请人：Epizyme, Inc.

  公开号：US20170305922A1

  公开（公告）日：2017-10-26

  Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein R1, R2a, R2b, R3 and Ring B are as defined herein, and Ring A is a group of Formula (A-i), (A-ii), or (A-iii): wherein R, R, R, R, and R are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
• FUMAGILLOL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME
  申请人：Zafgen, Inc.

  公开号：US20170342058A1

  公开（公告）日：2017-11-30

  Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
• RHO-ASSOCIATED PROTEIN KINASE INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND PREPARATION METHOD AND USE THEREOF
  申请人：BEIJING TIDE PHARMACEUTICAL CO., LTD.

  公开号：US20190276440A1

  公开（公告）日：2019-09-12

  The present invention relates to a Rho-associated protein kinase inhibitor of formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and a use of the same in preventing or treating a disease mediated by Rho-associated protein kinase (ROCK).