FIELD: organic chemistry. SUBSTANCE: invention relates to a method of synthesis of derivatives of taxanes of the general formula (I) by esterification of the protected baccatine (III) or protected 10-deacetylbaccatine (III) with acid of the general formula (II)
. In general formulas (I) and (II) Ar means phenyl; R1 and R2 have similar or different values and mean hydrogen atom, C1-C8-alkyl, C1-C8-alkoxyphenyl; R3 means acetyl or protective group of functional hydroxy-group and R4 means protective group of functional hydroxy-group; R means phenyl or radical of the formula R5--O- where R5 means direct or branched C1-C8-alkyl. Compounds of the general formula (I) can be used for preparing taxol, taxoter and their analogs that show the apparent antitumor activity. EFFECT: improved method of synthesis. 16 cl, 5 ex
Authors
Dates
1998-09-20—Published
1993-10-28—Filed