反应详情

Analogously to Example 1, 1.6 g of 1-{4-[N-(2-isopropoxyethyl)-N-chloroacetyl-amino]-benzoyl}-4-[2-(4-chlorophenyl)-ethyl]-piperazine--freed from the corresponding hydrochloride by treatment with a mixture of aqueous ammonia solution/methylene chloride--are reacted with 0.55 g of L-cysteinyl-glycine, yielding 1-{{4-{N-2-isopropoxyethyl)-N-[[[2R]-2-[N'-(carboxymethyl)carbamoyl]-2-amino-ethylmercapto-acetyl]]-amino}-benzoyl}}-4-[2-(4-chlorophenyl)-ethyl]-piperazine. The hemihydrate thereof has a melting point of 85°-87° and an αD25 =-1.5° (c=0.545%, methanol).