| 摘要 |
FIELD: chemical technology, pharmacy. SUBSTANCE: invention relates to a method of synthesis of (2R,3S)-3-tert.-butoxy- -carbonylamino-2-hydroxy-3-phenylpropionate-4-acetoxy--2alpha- -benzoyloxy-5beta,20-epoxy--1,7beta,10beta-trihydroxy-9-oxo-tax-11-ene--13alpha- -yl trihydrate that shows antitumor activity. Trihydrate has very low hygroscopicity as compared with other forms of this substance. Method of synthesis involves crystallization of (2R, 3S)-3-tert. -butoxycarbonylamino-2-hydroxy-3-phenyl- -propionate-4-acetoxy--2alpha-benzoyloxy--5beta,, 20-epoxy--1,7beta,10beta- -trihydroxy-9-oxo-tax-11-ene-13alpha-yl in a mixture of water and aliphatic alcohol containing 1-3 carbon atoms at weight ratio = 2:1 followed by drying of prepared product, mainly at 40 C, under pressure, mainly at 4-7 kPa, in atmosphere of relative humidity mainly about 80%. Crystallization process is carried out preferably in the presence of ascorbic acid. EFFECT: improved method of synthesis. 5 cl, 2 ex
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