| 摘要 |
FIELD: organic chemistry, chemical technology, medicine, antibiotics. ^ SUBSTANCE: invention relates to a method for synthesis of 14beta=hydroxybaccatin III-1,14-carbonate used in synthesis of novel taxane derivatives possessing an anti-tumor activity. Proposed method involves the following steps: (a) treatment of 7-triethylsilyl-13-ketobaccatin III of the formula: with suitable bases and oxidizing agents to yield 7-triethylsilyl-13-keto-14-hydroxybaccatin III of the formula: ; (b) carbonization of hydroxyl groups at positions 1 and 14 to yield 14beta-hydroxy-7-TES-13-ketobaccatin III-1,14-carbonate of the formula: ; (c) reduction of ketone at position 13, and (d) removal of a protective group at position 7. Also, invention relates to novel intermediate substances. Invention provides simplifying of the process and enhancing yield. ^ EFFECT: improved method of synthesis. ^ 10 cl, 1 ex |
