| abstract |
NEW MATERIAL:The amino acid derivative of formula I (R 1 and R 2 are OH, alkyloxy, aryloxy, aralkyloxy, alkyl, or arylaralkyl; R 3 , R 5 , R 8 and R 11 are H or alkyl; R 4 , R 6 , R 7 , R 9 and R 10 are H, alkyl, aryl or aralkyl; R 12 is OH, alkyloxy, aryloxy, aralkyloxy, amino, mono- or di-alkyl, -aryl or -aralkylamino; R 6 , R 7 , R 9 and R 10 may together form an alkylene bridge). n EXAMPLE: Dibenzylphosphoryl-L-alanyl-L-prolyl-L-proline L-arginine salt. n USE: Hypotensor. n PROCESS: The compound of formula I can be prepared e.g. by reacting the tripeptide derivative of formula II with the phosphoridate of formula III (e.g. phosphochloridate diester) in the presence of a base such as triethylamine to convert the N-terminal to phosphorus derivative, and if ncessary, eliminating the protecting group. n COPYRIGHT: (C)1984,JPO&Japio |