Daiichi Pharmaceutical Co., Ltd.

Akihiro Imura

Tsutomu Yagi

Yoshihiro Takayanagi

Kouji Sato

Keiji Nakayama

Katsuhiko Okano

Mikihiro Itoh

Yukinari Kobayashi

Tomoyuki Nagai

Tatsuya Yamaguchi

Seishiro Uchida

Yutaka Kitagawa

Kazuo Kubota

Shigeru Ichikawa

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

Treatment of a lactic acid ester derivative with an enzyme or the like, which has asymmetric ester-hydrolyzing ability, can specifically hydrolyze the ester moiety of an isomer existing as the pair to the racemic derivative. Use of the compound obtained by this hydrolysis makes it possible to produce an optically active propoxyaniline derivative by a shorter process than the conventional art 

Process for preparation of optically active propoxyaniline derivatives

Processes for producing antibacterial agents and intermediates useful in producing antibacterial agents are provided and include producing compound (VI-a) in accordance with the following reaction schema, as well as production intermediates thereof 

Process for producing benzoxazine derivative and production intermediate thereof

A process for producing a compound represented by the following formula (II) which comprises treating a compound represented by the following formula (I) (wherein R, Rand Rrepresent each a specific substituent) with an enzyme capable of asymmetrically hydrolyzing an ester and the novel compound (II). The process of the present invention makes it possible to easily obtain an optically active 2-azetidinone derivative in a large amount at a low cost 

Method for producing 2-azetidinone derivative

Processes for producing antibacterial agents and intermediates useful in producing antibacterial agents are provided and include producing compound (VI-a) in accordance with the following reaction schema, as well as production intermediates thereof.

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Edogawa-ku, Japan

Akihiro Imura