| 摘要 |
<p>PURPOSE:To provide a new pyrrolidine derivative useful as a synthetic intermediate for penem compound and carbapenem compound having excellent antibacterial activity. CONSTITUTION:A compound of formula I (Ph is phenyl; R is amino-protecting group; R1 is H, lower alkyl, lower alkenyl, etc.; R2 is lower alkyl, lower alkenyl, aralkyl, etc.; R1 and R2 may be bonded together to form an alkylene chain or together with N form a 4 to 7-membered cyclic amino, etc.) e.g. (2S,4S)-N,N- dimethyl-1-allyloxycarbonyl-4-benzoylthio-2-pyrrolidinecarboxamide. The compound can be produced by reacting a compound of formula II (X is active ester group of OH) with a thiobenzoic acid alkali metal salt (e.g. potassium salt) in an inert solvent (e.g. toluene-DMF) at 50-150 deg.C.</p> |
