tert-butyl (3,4-dimethylisothiazol-5-yl)carbamate | 174079-10-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: tert-butyl (3,4-dimethylisothiazol-5-yl)carbamate
• 英文别名: (3,4-Dimethyl-isothiazol-5-yl)-carbamic acid tert-butyl ester；tert-butyl N-(3,4-dimethyl-1,2-thiazol-5-yl)carbamate
• CAS: 174079-10-8
• 化学式: C₁₀H₁₆N₂O₂S
• 分子量: 228.315
• InChiKey: DLMYBLJTZJNYEV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  79.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl (3,4-dimethylisothiazol-5-yl)carbamate 在 三氟乙酸 作用下， 生成 3,4-Dimethyl-1,2-thiazol-5-amine
  参考文献：
  名称：

  Discovery and synthesis of a potent sulfonamide ETB selective antagonist

  摘要：

  The synthesis and structure activity relationships of a series of sulfonamide endothelin antagonists are described. In the course of our modification studies, we discovered ETB selective antagonists. The most potent compound 15f displays IC50 values of 1.7 mu M and 0.002 mu M to ETA and ETB receptors, respectively. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00366-8
• 作为产物：
  描述：

  3-(Boc-amino)-5-methylisothiazole 在 一氯化碘 、 sodium hydride 、 溶剂黄146 作用下， 以 四氢呋喃 为溶剂， 生成 tert-butyl (3,4-dimethylisothiazol-5-yl)carbamate
  参考文献：
  名称：

  Discovery and synthesis of a potent sulfonamide ETB selective antagonist

  摘要：

  The synthesis and structure activity relationships of a series of sulfonamide endothelin antagonists are described. In the course of our modification studies, we discovered ETB selective antagonists. The most potent compound 15f displays IC50 values of 1.7 mu M and 0.002 mu M to ETA and ETB receptors, respectively. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00366-8

文献信息

• PYRAZINE KINASE INHIBITORS
  申请人：Portola Pharmaceuticals, Inc.

  公开号：US20130131040A1

  公开（公告）日：2013-05-23

  Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

  提供了用于抑制Syk激酶的吡嗪化合物，用于制备这些化合物的中间体，它们的制备方法，药物组合物，抑制Syk激酶活性的方法，以及治疗至少在一定程度上由Syk激酶活性介导的疾病的方法。
• Pyrazine Kinase Inhibitors
  申请人：Portola Pharmaceuticals, Inc.

  公开号：US20140309209A1

  公开（公告）日：2014-10-16

  Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

  提供了吡嗪化合物，用于抑制Syk激酶，用于制备这些化合物的中间体，其制备方法，药物组合物，用于抑制Syk激酶活性的方法，以及用于治疗至少部分由Syk激酶活性介导的疾病的方法。
• US8877760B2
  申请人：——

  公开号：US8877760B2

  公开（公告）日：2014-11-04
• US9359308B2
  申请人：——

  公开号：US9359308B2

  公开（公告）日：2016-06-07
• COMPOUNDS, COMPOSITIONS AND METHODS OF USE TO TREAT HYPOPARATHYROIDISM AND OSTEOPOROSIS
  申请人：[en]SEPTERNA, INC.

  公开号：WO2024155601A1

  公开（公告）日：2024-07-25

  Disclosed are compounds that are parathyroid hormone receptor 1 agonists, and methods of using them for preventing or treating osteoporosis, fracture, osteomalacia, arthritis, thrombocytopenia, hypoparathyroidism, hyperphosphatemia or tumoral calcinosis.