| abstract |
NEW MATERIAL:The compound of formula I (R is -CH 2 -S-CH 3 , -CH 2 -CH 2 -CH 3 or group of formula II). n EXAMPLE: The compound of formula III. n USE: An anticarpaine compound. It exhibits strong enzymeinhibiting activity against carpaine, and little inhibiting activity to serine protease. n PREPARATION: The objective compound of formula I can be prepared by suspending the ester of formula IV (R' is methyl or ethyl) in a tert-alcohol, adding a reducing agent such as sodium borohydride, adding anhydrous methanol to the mixture under refluxing in an inert gas atmosphere, and oxidizing the resultant alcohol of formula V with sulfur trioxide-pyridine complex in dimethyl sulfoxide. The starting compound of formula IV is synthesized by conventional peptide synthesis using corresponding amino acids or peptides. n COPYRIGHT: (C)1986,JPO&Japio |