METHOD FOR PRODUCING 1-(1-TERT-BUTOXYCARBONYL-4-PIPERIDYLACETYL)-4-MESYLOXYPIPERIDINE AND 1-(1-TERT-BUTOXYCARBONYL-4-PIPERIDYLACETYL)-4-MESYLOXYPIPERIDINE

WIPO Patent Application WO/2019/142901

A1

The purpose of the present invention is to provide 1-(1-tert-butoxycarbonyl-4-piperidylacetyl)-4-mesyloxypiperidine having a low impurity content. This problem can be solved by a method for producing 1-(1-benzyl-4-piperidylacetyl)-4-hydroxypiperidine according to the present invention, comprising (1) a step for carrying out a reducing reaction of ethyl 1-benzyl-4-piperidylideneacetate represented by formula [1]: to obtain ethyl 1-benzyl-4-piperidylacetate represented by formula [2]: (2) a step for adding an aqueous ammonium chloride solution and an organic solvent to a liquid containing ethyl 1-benzyl-4-piperidylacetate, then mixing the reaction mixture, and separating the mixture into an organic layer and an aqueous layer: (3) a step for recovering ethyl 1-benzyl-4-piperidylacetate from the organic layer: and (4) a step for reacting the obtained ethyl 1-benzyl-4-piperidylacetate in the presence of a base with the 4-hydroxypiperidine represented by formula [3]: to obtaining 1-(1-benzyl-4-piperidylacetyl)-4-hydroxypiperidine represented by formula [4]: .

NAKAGAWA KIYONO (JP)
ITO YOSHIHIRO (JP)
KITAHARA HIROHISA (JP)

PCT/JP2019/001427

July 25, 2019

January 18, 2019

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YUKI GOSEI YAKUHIN KOGYO KK (JP)

C07D211/46; C07D211/34

WO2007111323A1	2007-10-04
WO2004031153A2	2004-04-15

JP2004131486A	2004-04-30
JP2005179351A	2005-07-07
JP2004182730A	2004-07-02
JP2003155287A	2003-05-27
JP2006104130A	2006-04-20
JP2004131486A	2004-04-30
JP4207201B2	2009-01-14

See also references of EP 3741743A4

YAMAGUCHI Kenjiro et al. (JP)

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