N-allyl-N-chloro-4-methylbenzenesulfonamide

• 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-allyl-N-chloro-4-methylbenzenesulfonamide
• 英文别名: N-allyl-N-chlorotosylamide；N-chloro-4-methyl-N-prop-2-enylbenzenesulfonamide
• 化学式: C₁₀H₁₂ClNO₂S
• 分子量: 245.73
• InChiKey: NWNKGJNINLAAOA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-allyl-N-chloro-4-methylbenzenesulfonamide 在 三乙基硼 、 环己烯 作用下， 以 正己烷 、 苯 为溶剂， 以100%的产率得到N-烯丙基对甲苯磺酰胺
  参考文献：
  名称：

  Radical [3 + 2] Annulation of N-Allyl-N-chlorotosylamide with Alkenes via Atom-Transfer Process

  摘要：

  [GRAPHICS]A radical [3+2] annulation reaction with an N-centered radical has been developed. The reaction of alkenes with N-allyl-N-chlorotosylamide yields the corresponding pyrrolidine derivatives in good yields in the presence of Et3B as a radical initiator.

  DOI：

  10.1021/ol016310j
• 作为产物：
  描述：

  N-烯丙基对甲苯磺酰胺 在 1,3-二氯-5,5-二甲基海因 作用下， 以 二氯甲烷 为溶剂， 生成 N-allyl-N-chloro-4-methylbenzenesulfonamide
  参考文献：
  名称：

  可见光驱动光催化促进N-杂螺环的多组分直接组装

  摘要：

  N-杂螺环是在天然产物和药物化合物中发现的有趣的结构单元，但其可靠的合成方法相对较少。在这里，我们利用光催化生成N-中心自由基，从N-烯丙基磺酰胺和烯烃构建β-螺环吡咯烷。已经以中等至非常好的产率构建了多种β-螺环吡咯烷，包括药物衍生物。产品的进一步衍生化也已被证明具有可行的放大程序，利用流动化学技术。

  DOI：

  10.1021/acs.joc.2c01684

文献信息

• Visible-Light-Mediated Annulation of Electron-Rich Alkenes and Nitrogen-Centered Radicals from <i>N</i>-Sulfonylallylamines: Construction of Chloromethylated Pyrrolidine Derivatives
  作者：Lorène N. S. Crespin、Andreas Greb、David C. Blakemore、Steven V. Ley

  DOI：10.1021/acs.joc.7b02146

  日期：2017.12.15

  A visible-light-mediated annulation of N-sulfonylallylamines and olefins is reported. Rapid access to highly functionalized chloromethylated pyrrolidines can be achieved using mild conditions for the generation of nitrogen-centered radicals. Both a transition-metal-based catalyst and an organic dye can be used as photosensitizers with 0.5 mol % loading. The reaction was found to be applicable to a

  报道了N-磺酰基烯丙基胺和烯烃的可见光介导的环化。使用温和条件生成氮中心自由基可以快速获得高度官能化的氯甲基化吡咯烷。过渡金属基催化剂和有机染料都可以用作具有0.5 mol％负载量的光敏剂。发现该反应适用于多种富电子和电子中性的烯烃。
• INHIBITORS OF CYCLIN DEPENDENT KINASES AND THEIR USE
  申请人：Lal Bansi

  公开号：US20070015802A1

  公开（公告）日：2007-01-18

  The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ic) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ic) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ic) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (Ic) either alone or in combination with another active agent, in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (Ic) either alone or in combination with another active agent, together with pharmaceutically acceptable carrier substances and auxiliary substances.

  本发明涉及一种新型化合物，用于抑制细胞周期蛋白依赖性激酶，特别是公式(Ic)的香豆素衍生物，其中R1、R2、R3、R4、R5、R6、R7和A的含义如权利要求所示。本发明还涉及制备公式(Ia)化合物的方法，抑制细胞周期蛋白依赖性激酶和抑制细胞增殖的方法，以及使用公式(Ic)化合物在治疗和预防细胞周期蛋白依赖性激酶抑制剂可治疗或预防的疾病，如癌症，以及使用公式(Ic)化合物制备应用于这些疾病的药物。本发明还涉及含有公式(Ic)化合物的组合物，单独或与另一种活性剂联合使用，与惰性载体混合或以其他方式与惰性载体相结合，特别是含有公式(Ic)化合物的药物组合物，单独或与另一种活性剂联合使用，以及与药用载体物质和辅助物质相结合。
• Inhibitors of Cyclin Dependent Kinases and Their Use
  申请人：Lal Bansi

  公开号：US20110136873A1

  公开（公告）日：2011-06-09

  The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (Ia) either alone or in combination with another active agent, in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (Ia) either alone or in combination with another active agent, together with pharmaceutically acceptable carrier substances and auxiliary substances.

  本发明涉及新型化合物，用于抑制细胞周期蛋白依赖性激酶，更具体地说，涉及公式(Ia)的香豆酮衍生物，其中R1、R2、R3、R4、R5、R6、R7和A具有所述权利要求中指示的含义。本发明还涉及制备公式(Ia)化合物的方法，抑制细胞周期蛋白依赖性激酶和抑制细胞增殖的方法，以及使用公式(Ia)化合物治疗和预防通过抑制细胞周期蛋白依赖性激酶治疗或预防的疾病，如癌症，使用公式(Ia)化合物制备应用于此类疾病的药物。本发明还涉及含有公式(Ia)化合物的组合物，单独或与另一活性剂混合，与惰性载体混合或以其他方式与惰性载体相关联，特别是含有公式(Ia)化合物的制药组合物，单独或与另一活性剂混合，以及与药物可接受的载体物质和辅助物质一起使用。
• US7271193B2
  申请人：——

  公开号：US7271193B2

  公开（公告）日：2007-09-18
• US7884127B2
  申请人：——

  公开号：US7884127B2

  公开（公告）日：2011-02-08