Nippon Kayaku Kabushiki Kaisha

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Masashi Nagai

Masatoshi Abe

Keiichirou Yamamoto

Hiroko Yamazaki

Seiichi Saito

Takashi Harada

Hideo Sugimura

Akira Shiozawa

Makoto Tsuda

Kazuhisa Narita

Yukihiro Sagawa

Takaaki Nishikiori

Tomio Morino

Tsugio Tomiyoshi

Takamichi Sato

Chihiro Nishimura

Yoshitaka Satoh

Atsushi Kuwahara

A method for preparing a compound represented by the following general formula (5)   A method for preparing an optically active intermediate of sulphostin or an analogue thereof, which is an optically active amine salt of an optically active compound represented by the following general formula (8) where n is integer of 0 to 3; Y represents protecting group for the amino group; and each configuration at C* and P* may be the same or different and indicates S or R, the method including reacting a compound represented by the following general formula (7) where n and Y are as described above; and the configuration of C* indicates either of S or R, with an optically active amine, and resolving the formed diastereomeric salt by fractional crystallization.

Method for preparing sulphostin and analogue thereof or preparation intermediate thereof

There are disclosed a novel &#x3b1;-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is &#x2014;(CH)&#x2014; wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.

&#x3b1;-Amino-N-(diaminophosphinyl)lactam derivatives

Process for producing novel naphthyridine derivatives

A novel cystacycline derivative which has an excellent effect of promoting the differentiation of neurons and is useful as a remedy for central nervous system disorders, a remedy for peripheral nerve disorders, etc.

Compound having effect of promoting neuron differentiation

This invention relates to a process for producing an optically active cyclobutylamine which comprises reacting a racemic modification of cyclobuthylamine represented by the following general formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 represent each a hydrogen atom or a protecting group; with an optically active N-acylphenylglycine to thereby give two corresponding diastereomeric salts, crystallizing the more difficultly soluble diastereomeric salt and isolating the corresponding optically active cyclobutylamine from the diastereomeric salt thus crystallized. The optically active substances of the compound of the above general formula [I] are useful as, for example, an intermediate in the synthesis of 9-[(1R, 2R, 3S)-2,3-bis(hydroxymethyl)-1-cyclobutyl]guanine which is expected as an antiviral agent.

Process for producing optically active cyclobutylamines

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Nishitokyo, Japan

Masashi Nagai