| 摘要 |
NEW MATERIAL:A guanidinobenzoic acid derivative of formula I (Z is carbon- carbon covalent bond; methylene, vinylene, etc.; R<1> and R<2> are H or lower alkyl groups), or its acid addition salt. EXAMPLE:p-( p-Guanidinobenzoyloxy )-N, N-dimethyl-phenylacetamido-methanesulfonate. USE:Remedies for acute pancreatitis, or hemorrhagic diseases as an aptiplasmin, having powerful inhibitory actions against proteolytic enzyme trypsin or plasmin at a low concentration, and high water solubility, usable for administration as an aqueous or physiological salt solution. PROCESS:An acid addition salt of a compound of formula II (X is halogen) is reacted with a compound of formula III in an inert solvent in the presence of a dehydrohalogenating agent at -20 deg.C to room temperature for 1-5hr to give the title derivative of formula I. |
