| 摘要 |
<p>NEW MATERIAL:The amino acid derivative of formula I (R1 and R2 are OH, alkyloxy, aryloxy, aralkyloxy, alkyl, or arylaralkyl; R3, R5, R8 and R11 are H or alkyl; R4, R6, R7, R9 and R10 are H, alkyl, aryl or aralkyl; R12 is OH, alkyloxy, aryloxy, aralkyloxy, amino, mono- or di-alkyl, -aryl or -aralkylamino; R6, R7, R9 and R10 may together form an alkylene bridge). EXAMPLE:Dibenzylphosphoryl-L-alanyl-L-prolyl-L-proline L-arginine salt. USE:Hypotensor. 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.</p> |
