Eisai Company, Limited

Kabushiki Kaisha Yakult Honsha

Takayuki Shioiri

Masanori Mizuno

Kunio Kado

Yasumasa Hamada

Naoko Irako

A process for the preparation of azide derivatives useful as drugs, perfumes or intermediates of dyes by reacting an alcohol derivative with di-p-nitrophenyl phosphorazidate in the presence of 1,8-diazabicyclo[5.4.0]-7-undecene.

Process for the preparation of azide derivatives

New proline derivatives of the general formula: ##STR1## wherein R stands for a lower alkyl group and X for a N-terminal protective group conventional in amino acid chemistry or an acyl group derived from an amino acid with a protective group at the N-terminal. They have inhibitory activity against prolylendopeptidase and are relatively chemically stable as compared with known compounds of this type.

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Aichi, Japan

Takayuki Shioiri