METHOD FOR SELECTIVE DERIVATIZATION OF TAXANES Russian patent published in 2004 - IPC

FIELD: organic chemistry of natural compounds, chemical technology. SUBSTANCE: invention relates to new acylation method of taxane hydroxyl group involving treatment of taxane with acylating agent taken among the group consisting of anhydrides, dicarbonates, thiodicarbonates and isocyanates in the reaction mixture comprising less of one equivalent of a base per each equivalent of taxane but preferably in the ratio = (1:1)-(1:100) to form C(10)-acylated taxane. Invention relates also to method for silylation of C(10)-hydroxyl group of taxane and methods for conversion of C(7)-hydroxyl group of 10-acyloxy-7-hydroxytaxane to acetal or ketal. Invention provides a new method for selective derivatization of taxanes by means C(10)-group is protected or derivatized before C(7)-hydroxyl group. EFFECT: improved derivatization method of taxanes. 32 cl, 2 tbl, 10 ex