摘要 |
1362696 Tripeptamide ABBOTT LABORATORIES 30 July 1971 [6 Aug 1970] 36063/71 Heading C2C Pyroglutamylhistidylproline amide is prepared by reacting a solution of pentachlorophenyl pyroglutamate in an inert, polar, organic solvent with an aqueous solution of one molar equivalent of histidine dissolved in an equimolar amount of an alkali metal hydroxide at 0-10‹ C. for 5-60 mins., adding to the reaction mixture at least one molar equivalent of proline amide hydrochloride at 0‹ C. to room temperature and after dissolution of the amide, adding 1-2 molar equivalents of an epimerization inhibitor, cooling the resulting mixture with agitation at 0‹ C., adding at least one molar equivalent of a solution of dicyclohexylcarbodiimide in an inert organic, polar solvent, and stirring the mixture at - 10‹ to + 10‹ C. for at least 10 hrs. |