Daiichi Pharmaceutical Co., Ltd.

Seishiro Uchida

Yoshihiro Takayanagi

Tatsuya Yamaguchi

Akihiro Imura

Makoto Ono

Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds. A compound of formula (1) (wherein Ris an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group; Ris a hydroxyl group optionally having a protective group) is processed with an alkali metal permanganate to produce a compound of formula (2), which may be a starting material for oral-administrable antitumor compounds. 

Method for producing pentacyclic taxans

A crystal of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylidenedioxy]-5,20-epoxy-1-hydroxytax-11-en-13-yl (2R,3S)-3-(tert-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate, which has characteristic peaks at diffraction angles (2&#x3b8;) of 6.2&#xb0;, 10.3&#xb0;, 10.7&#xb0;, 11.4&#xb0;, and 12.0&#xb0; in a powder X-ray diffraction pattern, and a method for preparing the aforementioned crystal, which comprises the step of performing crystallization by using an organic solvent selected from the group consisting of a ketone type solvent, a nitrile type solvent, and a mixture thereof, or a mixture of said organic solvent and water.

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Tokyo, Japan

Seishiro Uchida