| 摘要 |
NEW MATERIAL:The compound of formula I (R1 is straight or branched 1-6C alkyl, 3-6C cycloalkyl, etc.; R2 is H or alkoxy; excluding the case that R2 is H and R1 is methyl) and its acid addition salt. EXAMPLE:1-Methyl-4-[4-(7-methoxy-1, 2, 3, 4-tetrahydro-1-naphthoyloxy) benzoyl]- piperazine. USE:It has chymotrypsin-inhibiting activity and is useful as a remedy for pancreatic diseases, etc. PROCESS:The compound of formula I can be prepared by esterifying the 4-substituted phenol of formula II with the tetrahydronaphthyl-carboxylic acid of formula III. The esterification is carried out, e.g. by reacting the reactive derivative of the compound of formula III (e.g. acid halide, acid anhydride, etc.) with the compound of formula II, or by reacting the compound of formula II with the compound of formula III in the presence of a dehydrating agent such as DCC. |
