Trihydrate of (2R,3S)-4,10-diacetoxy-2alpha-benzoyloxy-5beta, 20-epoxy-1,7beta-dihydroxy-9-oxo-tax-11-en-13alpha-yl-3-benzoylamino-2-hydroxy-3-phenylpropionate and process for preparing thereof

摘要

In the present invention there is disclosed trihydrate of (2R,3S)-4,10-diacetoxy-2alpha-benzoyloxy-5beta, 20-epoxy-1,7beta-dihydroxy-9-oxo-tax-11-en-13alpha-yl-3-benzoylamino-2-hydroxy-3-phenylpropionate that is prepared by dissolving or suspending (2R,3S)-4,10-diacetoxy-2alpha-benzoyloxy-5beta, 20-epoxy-1,7beta-dihydroxy-9-oxo-tax-11-en-13alpha-yl-3-benzoylamino-2-hydroxy-3-phenylpropionate in excess of an aliphatic alcohol containing 1 to 3 carbon atoms, whereby 6 to 12 parts by weight of the aliphatic alcohol are used per one weight part of the (2R,3S)-4,10-diacetoxy-2alpha-benzoyloxy-5beta, 20-epoxy-1,7beta-dihydroxy-9-oxo-tax-11-en-13alpha-yl-3-benzoylamino-2-hydroxy-3-phenylpropionate, whereupon water is added to so obtained solution or suspension in such an amount that the weight ratio water/aliphatic alcohol is equal to 3 : 1 to 1 : 3. The crystallized (2R,3S)-4,10-diacetoxy-2alpha-benzoyloxy-5beta, 20-epoxy-1,7beta-dihydroxy-9-oxo-tax-11-en-13alpha-yl-3-benzoylamino-2-hydroxy-3-phenylpropionate is then separated and dried at pressure ranging from 1 to 7 kPa, at a temperature ranging from 30 to 50 degC and relative humidity within the range of 20 to 100 percent in order to obtain the trihydrate of the (2R,3S)-4,10-diacetoxy-2alpha-benzoyloxy-5beta, 20-epoxy-1,7beta-dihydroxy-9-oxo-tax-11-en-13alpha-yl-3-benzoylamino-2-hydroxy-3-phenylpropionate containing 5 to 7 percent by weight water.