| abstract |
NEW MATERIAL:A compound of formula I (R 1 is amino which may be acylated or protected; X is H, methoxy; W is H, sulfo). n EXAMPLE: (3S-4R)-3-amino-4-cyano-2-azetidinone. n USE: A useful intermediate in the synthesis of optically active 4-substituted-2-azetidinone with antibacterial and β-lactamase-inhibiting activities. The compounds with sulfo group as W has both above activities and are used a remedy for infections caused by gram-positive and -negative bacteria in mammarian animals including men. n PREPARATION: The reaction of a compound of formula II [R 2 is acylated or protected amino; Y is halogen, COOR 3 (R 3 is hydrocarbon), SCOR 3 ] with a cyanide is carried out, preferably in the presence of a phase-transfer catalyst, when needed, deprotected to give the compound of formula I . n COPYRIGHT: (C)1984,JPO&Japio |