4 ' manufacturing method null of - demethyl 4 formylmethyl 4 desokishi 4 epi- podophyllotoxin

摘要

PURPOSE: To obtain the derivative useful as an antitumor agent with a shortened reaction process without using toxic heavy metal as a reaction catalyst or causing the problems of waste water treatment, etc., by reacting a specific production intermediate with a specific vinyloxysilane derivative. ;CONSTITUTION: The derivative of the formula III, e.g. 4'-demethyl-4,4'-di-O-(2,2,2- trichloroethoxycarbonyl)-4-epipodophyllotoxin, is produced by reacting a 4'- demethyl-4-epipodophyllotoxin derivative of the formula I [R is OH-protecting group; R₁ is (halogen-substituted) lower alkyl or benzyl] with a vinyloxysilane derivative of the formula II (R₂ to R₄ are lower alkyl) preferably in the presence of a Lewis acid catalyst.;COPYRIGHT: (C)1995,JPO