N-[4-(5-oxooxolan-2-yl)phenyl]methanesulfonamide

• 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-[4-(5-oxooxolan-2-yl)phenyl]methanesulfonamide
• 化学式: C₁₁H₁₃NO₄S
• 分子量: 255.29
• InChiKey: JOYGQEGNSRFBEG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  80.8
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Compounds and methods for preparing methanesulfonamides
  申请人：——

  公开号：US20040167357A1

  公开（公告）日：2004-08-26

  A process for preparing (S)-(-)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide (IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[4-[ethyl(6-fluoro-6-metylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide (I) anll then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-lId.

  一种制备(S)-(-)-N-[4-[4-[乙基(6-氟-6-甲基庚基)氨基]-1-羟基]苯甲磺酰胺半富马酸盐的方法，包括在三乙酰氧硼氢化钠和乙酸乙酯存在下，将N-[4-(2S)-四氢-5-羟基-2呋喃基]苯甲磺酰胺(IIa)与氟胺(III)反应，得到[4-[4-[乙基(6-氟-6-甲基庚基)氨基]-1-羟基]苯甲磺酰胺(I)，然后将I转化为半富马酸盐Ia。还声明了制备IIa的方法以及中间体IIa-lId。
• COMPOUNDS AND METHODS FOR PREPARING METHANESULFONAMIDES
  申请人：PHARMACIA & UPJOHN COMPANY

  公开号：EP1395549A1

  公开（公告）日：2004-03-10
• US7232930B2
  申请人：——

  公开号：US7232930B2

  公开（公告）日：2007-06-19
• [EN] COMPOUNDS AND METHODS FOR PREPARING METHANESULFONAMIDES<br/>[FR] COMPOSES ET PROCEDES D'ELABORATION DE METHANESULFONAMIDES
  申请人：UPJOHN CO

  公开号：WO2002098845A1

  公开（公告）日：2002-12-12

  A process for preparing (S)-(-)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide (IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[-4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide (I) and then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-IId.