| 摘要 |
NEW MATERIAL:The compound of formula I [R1 and R2 are H or lower alkoxy; A is single bond, lower alkylene or lower alkenylene; R3 and R4 are lower alkyl or R3 and R4 together form lower alkylene; R5 is -X-(CO)n-Y (X is single bond, lower alkylene, etc.; n is 0 or 1; Y is H, cycloalkyl, aryl, etc.), etc.]. EXAMPLE:4-[4-( Carbamoylmethyl )piperidinocarbonylmethyl]phenyl 4-guanidino benzoate dihydrochloride. USE:It has the activity of proteolytic enzyme and is useful for the remedy of pancreatitis, thrombotic syndrome, etc. PREPARATION:The compound of formula I can be produced by carrying out dehydrative condensation of p-nitrobenzoic acid of formula II with the compound of formula III, reducing the resultant compound of formula IV to convert the nitro group to amino group and guanidinating the product. |
