| abstract |
NEW MATERIAL:A compound shown by formula I [R 1 is group shown by formu la II (R 6 is halogen, lower alkyl, benzyl, phenyl, etc.; Z is O or S), group shown by formula III, etc.; R 2 is H, lower alkyl, benzyl, methoxy, phenyl, etc.; R 3 is H, lower alkyl or R 2 and R 3 are bonded to form alicyclic 5- to 6-membered ring; R 4 and R 5 are lower alkyl or bonded to form cyclic structure such as pyrrolidine or piperidine]. n EXAMPLE: 5-(2-Piperidinomethyl)propionyl-3-phenylisoxazole. n USE: A central muscle relaxant and remedy for diabetic. n PREPARATION: According to the reaction formula, a compound shown by formu la IV is halogenated into a compound shown by formula V, which is then subjected to ring formation reaction with a compound shown by formula VI to give a compound. Further this compound is oxidized to give a compound shown by formula VII, which is reacted with a compound shown by formula VIII. This compound is aminomethylated to give a compound shown by formula I' (R 1 is group shown by formula II and Z is O in formula I). n COPYRIGHT: (C)1991,JPO&Japio |