bromomethyl methyl sulfone | 78967-61-0

• 分子结构分类: 有机化合物 - 有机硫化合物 - 磺酰类
• 英文名称: bromomethyl methyl sulfone
• 英文别名: Bromo(methanesulfonyl)methane；bromo(methylsulfonyl)methane
• CAS: 78967-61-0
• 化学式: C₂H₅BrO₂S
• mdl: MFCD20621856
• 分子量: 173.03
• InChiKey: ORVHFQDFCYNSQR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  6
• 可旋转键数：
  1
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  42.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  bromomethyl methyl sulfone 在 sodium azide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 azidomethyl-methyl sulfone
  参考文献：
  名称：

  [EN] 2-METHYL-4',5'-DIHYDROSPIRO[PIPERIDINE-4,7'-THIENO[2,3-C]PYRAN] DERIVATIVES AS INHIBITORS OF APOL1 AND METHODS OF USING SAME
  [FR] DÉRIVÉS DE 2-MÉTHYL-4',5'-DIHYDROSPIRO[PIPÉRIDINE-4,7'-THIÉNO[2,3-C]PYRAN] UTILISÉS EN TANT QU'INHIBITEURS DE APOL1 ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  The disclosure provides at least one compound, tautomer, deuterated derivative, or pharmaceutically acceptable salt chosen from compounds of Formula I, tautomers thereof, deuterated derivatives of those compounds or tautomers, and pharmaceutically acceptable salts of any of the foregoing, compositions comprising the same, and methods of using the same, including uses in treating APOL1-mediated diseases, including pancreatic cancer, focal segmental glomerulosclerosis (FSGS), and/or non-diabetic kidney disease (NDKD).

  公开号：

  WO2023154344A1
• 作为产物：
  描述：

  Bromdimethylsulfid 在 单过氧邻苯二甲酸 、 乙醚 作用下， 生成 bromomethyl methyl sulfone
  参考文献：
  名称：

  Boehme; Fischer; Frank, Justus Liebigs Annalen der Chemie, 1949, vol. 563, p. 54,64

  摘要：

  DOI：

文献信息

• Chemoselective mono halogenation of β-keto-sulfones using potassium halide and hydrogen peroxide; synthesis of halomethyl sulfones and dihalomethyl sulfones
  作者：N. Suryakiran、P. Prabhakar、T. Srikanth Reddy、K. Chinni Mahesh、K. Rajesh、Y. Venkateswarlu

  DOI：10.1016/j.tetlet.2006.11.129

  日期：2007.1

  The synthesis of alpha-halo beta-keto-sulfones using potassium halide and hydrogen peroxide as a chemoselective mono halogenation reagent and the synthesis of alpha, alpha-symmetrical and asymmetrical dihalo beta-keto-sulfones and alpha-halo, alpha-alkyl and beta-keto-sulfones is described. Base induced cleavage of alpha-halo beta-keto-sulfones, alpha,alpha-dihalo beta-keto-sulfones, and alpha-halo, alpha-alkyl beta-keto-sulfones afforded the corresponding halomethyl sulfones, dihalomethyl sulfones and haloalkyl sulfones. (c) 2006 Elsevier Ltd. All rights reserved.
• Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer
  作者：Fumiyuki Shirai、Anna Mizutani、Yoko Yashiroda、Takeshi Tsumura、Yuko Kano、Yukiko Muramatsu、Tsubasa Chikada、Hitomi Yuki、Hideaki Niwa、Shin Sato、Kenichi Washizuka、Yasuko Koda、Yui Mazaki、Myung-Kyu Jang、Haruka Yoshida、Akiko Nagamori、Masayuki Okue、Takashi Watanabe、Kouichi Kitamura、Eiki Shitara、Teruki Honma、Takashi Umehara、Mikako Shirouzu、Takehiro Fukami、Hiroyuki Seimiya、Minoru Yoshida、Hiroo Koyama

  DOI：10.1021/acs.jmedchem.0c00045

  日期：2020.4.23

  Tankyrases (TNKS/TNKS2) belong to the poly(ADP-ribose) polymerase family. Inhibition of their enzymatic activities attenuates the Wnt/beta-catenin signaling, which plays an important role in cancer pathogenesis. We previously reported the discovery of RK-287107, a spiroindoline-based, highly selective, potent tankyrase inhibitor. Herein we describe the optimization process of RK-287107 leading to RK-582, which exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered. In addition to the dose-dependent elevation and attenuation of the levels of biomarkers AXIN2 and beta-catenin, respectively, results of the TCF reporter and cell proliferation studies on COLO-320DM are discussed.
• Grosset, Stuart J.; Dubey, Pramod K.; Gill, Glen H., Canadian Journal of Chemistry, 1984, vol. 62, p. 798 - 807
  作者：Grosset, Stuart J.、Dubey, Pramod K.、Gill, Glen H.、Cameron, Stanley T.、Gardner, Patrick A.

  DOI：——

  日期：——
• GROSSERT, J. S.;DUBEY, P. K.;GILL, G. H.;CAMERON, T. S.;GARDNER, P. A., CAN. J. CHEM., 1984, 62, N 4, 798-807
  作者：GROSSERT, J. S.、DUBEY, P. K.、GILL, G. H.、CAMERON, T. S.、GARDNER, P. A.

  DOI：——

  日期：——
• Boehme; Fischer; Frank, Justus Liebigs Annalen der Chemie, 1949, vol. 563, p. 54,64
  作者：Boehme、Fischer、Frank

  DOI：——

  日期：——