Shionogi Company Limited

Toshiaki Masui

Kyozo Kawata

Makoto Kakinuma

Kazuhiro Yoshida

Takayuki Kasai

Disclosed is a process for the preparation of Compound (III), salt or solvate thereof by reacting Compound (I), salt or solvate thereof with Compound (II) in a toluene solvent in the presence of an additive such as water or an alcohol. Also disclosed is a process for the preparation of Compound (IV) comprising hydrolyzing the obtained Compound (III) if necessary, and then oxidizing. In the formula, Ris hydrogen, optionally substituted lower alkyl, optionally substituted aryl or optionally substituted aryl lower alkyl, and Ris optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aryl lower alkyl.

Process for the preparation of sulfomate-carboxylate derivatives

A process for producing amidine derivatives represented by the following reaction scheme, characterized in that the reactions of steps 1 and 3 are conducted in acetonitrile and the reaction of step 2 is conducted in acetone.

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Hyogo, Japan

Toshiaki Masui