Enolicam sodium, CGS-5391B(anhydrous)

7-氯-4-[(3,4-二氯苯基)氨基甲酰]-1,1-二氧代-2,3-二氢苯并[b]硫杂卓-5-醇钠水合物 依诺利康Chemical Name: 3',4',7-Trichloro-2,3-dihydro-5-hydroxy-1-benzothiepin-4-carboxanilide 1,1-dioxide monosodium salt monohydrate; 7-Chloro-N-(3,4-dichlorophenyl)-2,3-dihydro-5-hydroxy-1-benzothiepin-4-carboxamide 1,1-dioxide monosodium salt monohydrate
CAS No. 73574-69-3, 59756-39-7 (anhydrous), 59755-82-7 (anhydrous, free acid)
项目整合开发状态: Biological Testing
项目研究机构: Novartis (Originator)
合成路线:The oxidation of 7-chloro-5-hydroxy-2,3-dihydro-1-benzothiepin (I) with H2O2 in acetic acid - water gives 7-chloro-5-hydroxy-2,3-dihydro-1-benzothiepin-1,1-dioxide (II),which by reaction with pyrrolidine (III) and p-toluenesulfonic acid in refluxing benzene is converted into 7-chloro-5-pyrrolidino-2,3-dihydro-1-benzothiepin-1,1-dioxide (IV).The condensation of (IV) with 3,4-dichlorophenyl isocyanate (V) in hot THF yields N-(3,4-dichlorophenyl)-7-chloro-5-pyrrolidino-2,3-dihydro-1-benzothiepin-4-carboxamide-1,1-dioxide (VI),which is finally hydrolyzed with HCl in refluxing ethanol - water.