| 摘要 |
PURPOSE:To readily produce a beta-lactam-based antibiotic and a beta-lactam compound as a raw material for beta-amino acids in one process from an inexpensive allyl alcohol derivative. CONSTITUTION:An allyl alcohol derivative of formula I (R<1> is lower alkyl or aryl; R<2> and R<3> are H or lower alkyl; R<4> is H or lower alkyl or protected OH) is made to react with an imine compound of formula II (R<5> is lower alkyl, alkenyl, alkynyl, aryl, aromatic heterocyclic group, benzoyl or lower alkyloxycarbonyl which may have a substituent group, respectively; R<6> is lower alkyl or aryl which may have a substituent group, respectively) in the presence of carbon monoxide gas and a palladium catalyst to provide the objective beta- lactam compound of formula III. The compound of formula I used as a starting raw material can be synthesized by reacting a compound of formula IV with a dialkyl chlorophosphate or diaryl chlorophosphate in the presence of a base. |
