| 摘要 |
organic synthesis. SUBSTANCE: invention provides novel taxane derivatives of general formula 3b: (3b), in which R1,R2,R4,R6, and R14, independently from each other, denote H, OH, R, OR, OCOR, or OCOOR, wherein R independently denote linear or branched alkyl, aryl, or arylalkyl, which are prepared by rapidly adding, at temperature above room temperature, preferably between 20 and 80 C, corresponding 2-substituted alkoxycarbonyl chloride diluted in suitable solvent to vigorously stirred solution of 7,10-dihydroxytaxane of general formula 3a: (3a), which carries group OTcBoc in position 7 and R1,R2,R4,R6 and R14/ have the same meanings as indicated above, in presence of pyridine and/or sterilely hindered substituted pyridine, e.g. 4-pyrrolidinopyridine or dimathylaminopyridine. Invention also relates to compounds 3c: (3c). All these compounds are novel intermediates for taxanes depicted by general formula 3d: (3d), in which R1 and R2,R4R5R6 and R14 have the same meanings as indicated above, R10 denotes acyl O-CO-R (R as above), and R13/ is radical precursor of side chain of taxane. Compounds 3d are useful as antitumor agents. EFFECT: invention provides new way for synthesis of 10-deacetylbaccatin III substituted in position 7 with high selectivity. 12 cl, 1 tbl, 9 ex
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