N-methyl-N'-benzenesulfonylacetamidine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-methyl-N'-benzenesulfonylacetamidine
• 英文别名: N-(benzenesulfonyl)-N'-methylethanimidamide
• 化学式: C₉H₁₂N₂O₂S
• 分子量: 212.272
• InChiKey: YOAMRMXDMQQTFD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  66.9
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  苯磺酰基叠氮化物 、 1-(甲基氨基)乙硫酮 以 乙醇 为溶剂， 反应 3.0h， 以94%的产率得到N-methyl-N'-benzenesulfonylacetamidine
  参考文献：
  名称：

  Coupling reaction of thioamides with sulfonyl azides: an efficient catalyst-free click-type ligation under mild conditions

  摘要：

  我们报道了一种在没有任何活化添加剂的情况下，硫酰胺与磺酰叠氮进行耦合反应生成磺酰亚胺的方法。该反应在温和条件下于多种溶剂中进行。其中，水的效率表现最高。

  DOI：

  10.1039/c3cc46055j

文献信息

• DERIVATIVES OF AN FGFR INHIBITOR
  申请人：Incyte Corporation

  公开号：US20210171522A1

  公开（公告）日：2021-06-10

  The present disclosure relates to derivatives (e.g., hydroxyl, keto, glucuronide, sulfonic acid, and deuterated) of a Fibroblast Growth Factor Receptors (FGFR) inhibitor, including methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of FGFR mediated disease such as cancer.

  本公开涉及一种成纤维细胞生长因子受体（FGFR）抑制剂的衍生物（例如，羟基，酮基，葡萄糖醛酸盐，磺酸盐和氘代物），包括其制备方法以及在制备过程中有用的中间体，这些衍生物在治疗FGFR介导的疾病如癌症方面是有用的。
• JAK KINASE INHIBITOR, PREPARATION METHOD FOR SAME, AND APPLICATIONS THEREOF IN FIELD OF MEDICINE
  申请人：Shanghai Synergy Pharmaceutical Sciences Co., Ltd

  公开号：EP3939979A1

  公开（公告）日：2022-01-19

  Related are a JAK kinase inhibitor, a preparation method for same, and applications thereof in the field of medicine, related to the field of medicinal chemistry. Provided is a novel small molecule JAK inhibitor, which has the structure as represented by formula (II). The compound provides improved efficacy and safeness in preventing or treating a JAK-related indication.

  涉及一种JAK激酶抑制剂、其制备方法及其在医药领域的应用，与药物化学领域相关。本发明提供了一种新型小分子 JAK 抑制剂，其结构如式 (II) 所示。该化合物在预防或治疗 JAK 相关适应症方面具有更好的疗效和安全性。
• 4,6-pyrimidinylene derivatives and uses thereof
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US10695346B2

  公开（公告）日：2020-06-30

  The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., lung cancer, breast cancer, leukemia, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase (e.g. a protein kinase (e.g. a cyclin-dependent kinase (CDK) (e.g. CDK7, CDK12, or CDK13) or a lipid kinase such as a phosphatidylinositol-5-phosphate 4-kinase (PIP4K) (e.g., PI5P4Kα, PI5P4Kβ, or PI5P4Kγ)) in the subject.

  本发明提供了新颖的式(I)化合物及其药学上可接受的盐、溶液剂、水合物、多晶型、共晶体、同分异构体、立体异构体、同位素标记的衍生物、原药及其组合物。还提供了涉及本发明化合物或组合物的方法和试剂盒，用于治疗或预防受试者的增殖性疾病（如癌症（如肺癌、乳腺癌、白血病、淋巴瘤、黑色素瘤、多发性骨髓瘤、尤文氏肉瘤、骨肉瘤、脑癌、神经母细胞瘤）、良性肿瘤、血管生成、炎症性疾病、自身炎症性疾病和自身免疫性疾病）。使用本发明的化合物或组合物治疗患有增殖性疾病的受试者，可抑制激酶（如蛋白激酶（如细胞周期蛋白依赖性激酶（CDK）（如 CDK7、CDK12 或 CDK13）或脂质激酶，如磷脂酰肌醇-5-磷酸 4-激酶（PIP4K）（如、PI5P4Kα、PI5P4Kβ 或 PI5P4Kγ））。
• JP6112659
  申请人：——

  公开号：——

  公开（公告）日：——
• 4,6-PYRIMIDINYLENE DERIVATIVES AND USES THEREOF
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US20180110778A1

  公开（公告）日：2018-04-26

  The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., lung cancer, breast cancer, leukemia, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase (e.g. a protein kinase (e.g. a cyclin-dependent kinase (CDK) (e.g. CDK7, CDKl2, or CDKl3) or a lipid kinase such as a phosphatidylinositol-5-phosphate 4-kinase (PIP4K) (e.g., PI5P4Kα, PI5P4Kβ, or PI5P4Kγ)) in the subject.