PURPOSE: To obtain β-lactam useful as an antibiotic by reacting an N, N-di- protected glycine ester with an imine in the presence of a metal compd.
CONSTITUTION: A R2', R3', N-glycine represented by formula I (wherein R12 is a 1-8C alkyl or a 1-18C aryl; and R2' and R3' are same to R2 and R3 and form a ring along with N) and an imine represented by formula II (wherein R4' is same to R4; and R1' is same to R1) are reacted in the presence of an alkali metal base and a metal compd. represented by formula III (wherein M is Zn, Al or Zr; X, Y and Z are each a 1-8C alkyl, a 1-18C aryl or a halide; and (a), (b), (c) and (m) are 0-1 and either one of (a), (b) and (c) is 1 and (n) is 1-6) in a polar solvent (e.g.; diethyl ether) to obtain the objective substance represented by formula IV (wherein R2 and R3 are each H, a 1-8C alkyl or a 1-18C aryl; R1 is H, a halogen or a 1-8C alkyl and R4 is a 1-8C alkyl, hydroxy or a halogen). The metal compd. of the catalyst is used in an amt. less than that of the compd. represented by formula I to perform reaction.
FUREDERITSUKU HENDORITSUKU FUA
YOHAN TENSU BARUTOORUTO HEINRI