PURPOSE: To obtain the subject compound useful as an antimicrobial agent, an antitumor agent and a therapeutic agent for AIDS.
CONSTITUTION: A compound of formula I [R1 is H or amino-protecting agent; R2 is H, (substituted) alkyl or R2 and R3 are bonded together with N(CH2)mCH group to form 5-to 6-membered ring amino group; R4 is H or lower alkyl; X is H or halogen; (m) is 0-1; (n) is 1-2] such as (3'S)-7-[3-[(N-tert-butoxycarbonyl- L-alanyl)amino]-1-pyrrolidinyl]-6-fluoro-1-methyl-4-oxo-1H,4H-[1,31 thiazeto[3,2- a]quinoline-3-carboxylic acid ethyl ester. The compound of formula I is obtained by reacting a compound of formula II or formula III with an active compound, derived from an N-protected amino acid of formula IV (R5 is amino-protecting group), in a solvent optionally in the presence of a base and then optionally deprotecting or hydrolyzing.
KATO HIDEO
YASUDA SHINGO
YOSHIDA TOSHIHIKO
YAMAMOTO YOICHI
