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Title:
METHOD FOR PRODUCING HETEROCYCLIC COMPOUND
Document Type and Number:
WIPO Patent Application WO/2017/065287
Kind Code:
A1
Abstract:
The present invention provides a production method suitable for the production of a heterocyclic compound having an excellent CH24H-inhibiting activity on an industrial scale. In the present invention, 2-halogenonicotinic acid, a reactive derivative of 2-halogenonicotinic acid or a salt of 2-halogenonicotinic acid or the reactive derivative is reacted with a 4-benzyl-4-hydroxypiperidic acid addition salt to produce (4-benzyl-4-hydroxypiperidin-1-yl) (2-halogenopyridine-3-yl)methanone or a salt thereof, and subsequently the compound or the salt thereof is reacted with pyridine-4-boronic acid, a reactive derivative of pyridine-4-boronic acid or a salt of pyridine-4-boronic acid or the reactive derivative in the presence of a metal catalyst and a base to produce (4-benzyl-4-hydroxypiperidin-1-yl) (2,4'-bipyridin-3-yl)methanone or a salt thereof.

Inventors:
KOMURA FUMIYA (JP)
HIGUCHI YOSHIHIRO (JP)
Application Number:
PCT/JP2016/080581
Publication Date:
April 20, 2017
Filing Date:
October 14, 2016
Export Citation:
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Assignee:
TAKEDA PHARMACEUTICALS CO (JP)
International Classes:
C07D401/06; C07D401/14; C07B61/00
Domestic Patent References:
WO2006071958A12006-07-06
Foreign References:
JP2014528904A2014-10-30
JP2006527262A2006-11-30
JP2014506253A2014-03-13
JPH0585986A1993-04-06
Other References:
GOULD, PHILIP L.: "Salt selection for basic drugs", INTERNATIONAL JOURNAL OF PHARMACEUTICS, vol. 33, 1986, pages 201 - 217, XP025813036, ISSN: 0378-5173
AKIRA SUZUKI: "Suzuki-Miyaura Coupling (SMC) Hanno no Mondaiten", TCI MAIL, 2009, pages 2 - 23, XP009509604, ISSN: 1349-4856
Attorney, Agent or Firm:
TAKASHIMA, Hajime (JP)
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