Yuki Gosei Kogyo Co., Ltd.

Kiyono Nakagawa

Yoshihiro Ito

Yukiko Takeda

Hiromi Ishikawa Ishikawa

Yumiko Tanaka

Hirohisa Kitahara

The object of the present invention is to provide 1-(1-tert-butoxycarbonyl-4-piperidylacetyl)-4-mesyloxypiperidine having a low content of impurities The object can be solved by a method for preparing 1-(1-benzyl-4-piperidylacetyl)-4-hydroxypiperidine, comprising the steps of: to obtain 1-benzyl-4-piperidyl acetic acid ethyl ester represented by the formula [2]: in the presence of base, to obtain 1-(1-benzyl-4-piperidylacetyl)-4-hydroxypiperidine represented by the formula [4]:

Method for preparing 1-(1-tert-butoxycarbonyl-4-piperidylacetyl)-4-mesyloxypiperidine and 1-(1-tert-butoxycarbonyl-4-piperidylacetyl)-4-mesyloxypiperidine

The object of the present invention is to provide a simple method for preparing an N-alkoxycarbonyl piperidine derivative. The object can be solved by a method for preparing a hydroxypiperidine derivative, comprising a step of: wherein Ris an aralkyl group which may have a substituent group, and Ris an alkyl group, with 4-hydroxypiperidine in the presence of base, to obtain a hydroxypiperidine derivative represented by the formula (2) or the formula (3): wherein Ris an aralkyl group which may have a substituent group.

Method for preparing N-alkoxycarbonylpiperidine derivative, and intermediate therefor

The object of the present invention is to provide a method for preparing 4-(piperidin-4-yl)morpholine, which is easy to operate. The object can be solved by a method for preparing 4-(1-benzylpiperidin-4-yl)morpholine, characterized in that 5-fold molar or more of morpholine is added to 1-benzyl-4-piperidone, and the mixture is reacted with hydrogen under 1 MPa or less in the presence of platinum catalyst or palladium catalyst.

Method for preparing 4-(piperidin-4-yl)morpholine

A method of producing an N-alkoxycarbonylpiperidine derivative, comprising reacting an N-aralkylpiperidine derivative represented by the following general formula (1):wherein Rrepresents an aralkyl group which may have a substituent, with a mesyl halide in the presence of a base, thereby obtaining a mesylated product represented by the following general formula (2):wherein Rrepresents an aralkyl group which may have a substituent and Ms represents a mesyl group, and

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Tokyo, Japan

Kiyono Nakagawa