Nippon Kayaku Kabushiki Kaisha

Kouichi Ohkawa

Yoshinobu Miyazawa

Hitoshi Sato

Hiroshi Yoshikawa

Noriko Tomiyoshi

Taichi Koshigoe

Jouji Sekine

Shinichiro Saeki

Process for producing optically active cyanohydrins

An etoposide phosphate represented by the formula ##STR1## is prepared by blocking the hydroxyl groups of the saccharide moiety of etoposide with halogenoacetyl groups, thereafter phosphorylating the 4'-position, and removing the halogenoacetyl groups from the obtained phosphate in the presence of an amine. This process can give the objective etoposide phosphate in a higher yield than that of the prior art to enable the industrial mass-production thereof.

Process for the preparation of etoposide phosphate and intermediate

An etoposide phosphate represented by the formula (1): ##STR1## is prepared by blocking the hydroxyl groups of the saccharide moiety of etoposide with halogenoacetyl groups, thereafter phosphorylating the 4'-position, and removing the halogenoacetyl groups from the obtained phosphate in the presence of an amine. This process can give the objective etoposide phosphate in a higher yield than that of the prior art to enable the industrial mass-production thereof.

Etoposide phosphate and preparative intermediates

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Chiba, Japan

Kouichi Ohkawa