Rilmazafone hydrochloride dihydrate, 450191-S, Rhythmy

利马扎封盐酸盐 利马扎封 Chemical Name: 5-[[(Aminoacetyl)amino]methyl]-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1H-1,2,4-triazole-3-carboxamide monohydrochloride dihydrate; 1-[2-(o-Chlorobenzoyl)-4-chlorophenyl]-5-(glycylaminomethyl)-3-dimethylcarbamoyl-1H-1,2,4-triazole monohydrochloride dihydrate; 2',5-Dichloro-2-[3-dimethylcarbamoyl-5-(glycylaminomethyl)-1H-1,2,4-triazol-1-yl]benzophenone monohydrochloride dihydrate
CAS No. 85815-37-8 (anhydrous), 99593-25-6 (free base, anhydrous)
项目整合开发状态: Launched-1989
项目研究机构: Shionogi (Originator)
合成路线:The condensation of 2',5-dichloro-2-aminobenzophenone (I) with N,N-dimethyl-2-chloroacetoacetamide (II),by means of NaNO2 HCl in water acetone gives N,N-dimethyl-2-chloro-2-[2-(2-chlorobenzoyl)-5-chlorophenylazo]acetoacetamide (III),which by a treatment with aqueous NH3 in ethyl acetate is converted into N,N-dimethyl-2-amino-2-[2-(2-chlorobenzoyl)-5-chlorophenylazo]acetamide (IV).The cyclization of (IV) with phthalylglycylglycyl chloride (V) in THF-HMPT affords 2',5-dichloro-2-[3-dimethylcarbamoyl-5-(phthalylglycylaminomethyl)-1H-1,2,4-triazol-1-yl]benzophenone (VI),which is finally deprotected by a treatment with hydrazine in refluxing ethanol,and with HCl in the same solvent.