| abstract |
NEW MATERIAL:The compound of formula [R 1 and R 2 are H or methyl; R 3 is -CH 2 CH(CH 3 ) 2 , -CH 2 CH 2 SCH 3 , etc.; X is L(D)-arginine; Tyr is tyrosine; Gly is glycine]. n EXAMPLE: Tyrosyl-D-arginyl-glycyl-N-methylphenylalanyl-leucinol. n USE: Long-acting analgesic. n PROCESS: For example, benzyloxycarbonyl-tyrosyl-D-arginyl-mesitylene-2-sulfonyl- hydrazide, etc. are dissolved in DMF, etc., and added with hydrochloric acid, isoamyl nitrite, etc. under cooling. The mixture is made to react with glycine, etc. in the presence of an alkali, mixed with DMF solution of N-methylphenylalanyl- leucinol, etc., cooled, and made to react with triethylamine, 1-hydroxybenzotriazole, and dicyclohexylcarbodiimide by adding the compound in the order. n COPYRIGHT: (C)1982,JPO&Japio |