Optically pure camptothecin analogues

摘要

Two optically pure beta-hydroxy lactone camptothecin analogs (+)-5-ethyl-9,10-difluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7)indolizino(1,2-b)quinoline-3,15-dione (I) and (+)-9-chloro-5-ethyl-5-hydroxy-10-methyl-12-(4-methylpiperidinomethyl)-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7)indolizino(1,2-c)quinoline-2,15-dione (II), as well as one of its salts, (+)-1-(9-chloro-5-ethyl-5-hydroxy-10-methyl-3,15-dioxo-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7)indolizino(1,2-b)quinoline-12-yl methyl)-4-methyl-hexahydropyridinium chloride (III) and intermediates (M) are new. Optically pure beta-hydroxy lactone camptothecin analogs of formulae (I) and (II), as well as salts of (II) of formulae (III) are new. Independent claims are also included for industrial intermediates of formula (M) and their preparation. R = 1-10C alkyl, especially ethyl.