| 摘要 |
<p>NEW MATERIAL:A guanidinobenzoic acid derivative of formula I: (Z is methylene, ethylene, or viylene group) and its acid salt. EXAMPLE:P-(P-Guanidinobenzoyloxy) benzoic acid. USE:Remedies for acute pancreatitis, hemorrhagic diseases, etc., having a powerful inhibitory actions on proteolytic enzymes trypsin and plasmin. PROCESS:An acid salt of a compound of formula II: (x is halogen) is reacted with a compound of formula III: (R is H, protective group for carboxylic acid) in the presence of a dehydrohalogenating agent in an inert solvent at-20 deg.C-room temperature for 1-5 hr, and the protective group R for the carboxylic acid is removed, if present, to give the compound of formula I. The starting acid salt can be obtained by heating P-guanidinobenzoic acid with thionyl chloride.</p> |
