Taisho Pharmaceutical Co., Ltd.

Tomomichi Yoshida

Kazuyuki Tomisawa

Takehiro Amano

Chihiro Yokoo

Kazuto Sekiuchi

Masami Goi

Dai Tatsuta

Masahiro Hasegawa

The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein Rrepresents a protecting group for an &#x3b1;-amino group, and Rrepresents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.

Method for production of cis-4-fluoro-L-proline derivatives

A process for preparing erythromycin A oxime or a salt thereof which comprises reacting erythromycin A with hydroxylamine using an acid, is disclosed. Erythromycin A oxime and the salts thereof are useful as intermediates for the synthesis of macrolide antibiotics.

Process for preparing erythromycin A oxime or a salt thereof

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Tokyo, Japan

Tomomichi Yoshida