Mitsui Chemicals, Inc.

Hiroki Ishibashi

Yasushi Fukuiri

Toshihiro Oikawa

Tomoyuki Ando

Hironori Komatsu

Kiyoteru Nagahara

Yasuko Matsuba

Tadashi Araki

Katsutoshi Tsuchiya

Atsushi Sakuma

Kaori Matoishi

Toshifumi Yamaki

Hitoki Miyake

Hideki Umetani

Kazuhiko Togashi

Reiko Abe

Ichirou Ikeda

Tsuneji Suzuki

Tsuyoshi Inoue

Takeshi Nakamura

Toshiyuki Kouno

Hiroharu Tanikawa

Katsuyuki Takahashi

The invention provides a method for producing a cytosine nucleoside compound from pentose-1-phosphate and cytosine or a derivative thereof using a nucleoside phosphorylase reactive to cytosine or a bacterium having the enzyme activity. The invention also provides a method for specifically reducing an activity to degrade the substrates or the product, resulting in efficient production of the cytosine nucleoside compound. According to the invention, little by-product is produced in producing cytonucleocide compounds.

Method for producing cytosine nucleoside compounds

A novel gluconate dehydratase derived fromand a gene encoding the gluconate dehydratase are provided. By reacting the gluconate dehydratase or a transformed cell containing the gene with an aldonic acid, the corresponding 2-keto-3-deoxyaldonic acid can be efficiently produced.

Gluconate dehydratase

A protected 2'-deoxycytidine is purified by precipitating the protected 2&#x2032;-deoxycytidine represented by general formula (3) in the form of a hydrated crystal from a solution containing the protected 2&#x2032;-deoxycytidine and water, and by recovering the protected 2&#x2032;-deoxycytidine:wherein R1 represents a 4-methoxytrityl, 4, 4&#x2032;-dimethoxytrityl, or triphenylmethyl group; and B1 represents a cytosine group having a protected amino group. The compound represented by general formula (3) is, in particular, a protected 2&#x2032;-deoxycytidine represented by formula (4):The 2&#x2032;-deoxycytidine is used as a raw material for antisense DNA.

Method for purifying protected 2'-deoxycytidines and hydrated crystals thereof

This invention provides a method for efficiently purifying 5'-protected thymidines which cannot be efficiently purified by the prior art. Impurities can be separated by obtaining crystals including a carbonyl-containing solvent to provide a highly pure 5&#x2032;-protected thymidine. Thus, this invention allows 5&#x2032;-protected thymidines, which cannot be purified in an industrial scale by the prior art, to be easily provided with a high purity in a large scale.

Method for purifying 5' -protected thymidines and novel derivatives thereof

In the case that a selectively monoacylated phenylenediamine derivative which is useful as any of medicines, agricultural chemicals, animal drugs and the intermediates of chemicals is prepared by reacting a benzoic acid derivative with a phenylenediamine derivative, the benzoic acid derivative is converted into a benzoyl imidazole derivative and this benzoyl imidazole derivative is then reaction with the phenylenediamine derivative, whereby the improvement of a preparation efficiency and the high selectivity of the monoacylation can be achieved, the steps of protection and deprotection being omitted.

Method of producing benzamide derivatives

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Fukuoka, Japan

Hiroki Ishibashi