Taisho Pharmaceutical Co., Ltd.

Mercian Corporation

Joji Sasaki

Sadafumi Omura

Takashi Adachi

Kazutoshi Mizoue

Takaaki Ishii

Shigeo Morimoto

Rokuro Okamoto

Koji Takeda

Kazuhiko Okamura

Hiroaki Kamiyama

Takatoshi Nagate

Motoko Oshida

Akiko Mikami

Mitsuaki Hirotsuka

Kiyoshi Kimura

There is provided a process for producing a bicyclo [3.1.0] hexane derivative represented by the formula (I) and a salt thereof including; causing an enzyme to act on an optically inactive compound represented by the formula (II) causing an asymmetric acylation reaction and a highly-stereoselective conversion to an optically active compound represented by the formula (III); and converting the compound represented by the formula (III) to the compound represented by the formula (I) or a salt thereof. 

Process for producing optically active bicyclo [3.1.0] hexane derivative using enzyme

Production of a bicyclo[3.1.0]hexane derivative, useful as a metabotropic glutamate receptor modulator, becomes possible by a production method that includes converting a compound represented by Formula (II) into a compound represented by Formula (III) by reaction with an acyl group donor in the presence of a microorganism-derived enzyme, without using an expensive optically active trans hydroxy ester as a starting material and without employing a fluorination reaction requiring an ultralow temperature reaction. Furthermore, since asymmetric synthesis can be carried out in a stage closer to the final product, the production method is useful as a production method that can mass produce a bicyclo[3.1.0]hexane derivative. 

Method of producing bicyclo[3.1.0] hexane derivative using enzyme

A method for introducing hydroxyl groups into vitamin D compound at the 1.alpha.- and/or 25-positions in the presence of a cyclodextrin compound by the use of a reaction mixture containing a microorganism being capable of hydroxylating vitamin D compound or a enzyme produced from the microorganism, is disclosed.

Method for the biological preparation of hydroxyvitamin D compounds

Mucor circinelloides f. griseo-cyanus IFO 4563 is cultivated in a medium containing 6-O-methylerythromycin A as a substrate to obtain 14-hydroxy-6-O-methyl-erythromycin A. This compound and its salt have anti-bacterial activity.

Process for preparing 14-hydroxy-6-O-methyl-erythromycin A

A method for introducing hydroxyl groups into vitamin D compounds at 1.alpha.- and/or 25-positions by use of a solution containing the mycelium of Actinomycetales being capable of hydroxylating vitamin D compound or the enzyme produced from the mycelium, is disclosed.

Method for preparing vitamin D compounds

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Omiya, Japan

Joji Sasaki