Method for producing sulfonyl chloride compound

Japanese Patent JP6343600

B2

An object of the present invention is to provide a production method of an intermediate used in the production method of a sulfonylpyrrole compound useful as a pharmaceutical product. The present invention relates to a method of producing sulfonylpyrrole compound (VI) by reacting a pyridine-3-sulfonic acid compound with phosphorus pentachloride in a solvent of chlorobenzene or trifluoromethylbenzene to give a pyridine-3-sulfonyl chloride compound, reacting the compound without isolation with compound (III) to give compound (IV), and subjecting the compound (IV) to a reductive amination reaction. wherein R 2 is a hydrocarbon group etc. and R 3 and R 4 are each a hydrogen atom etc., wherein R 1 is an optionally substituted pyridin-3-yl group, and the other symbols are as defined above, wherein R 5 is an alkyl group and the other symbols are as defined above.

JP2009508809	RAC-1 GTPase GTPase Inhibitors, Their Usage and Crystal Structure
WO/2018/229784	PHARMACEUTICAL COMPOSITIONS OF DABIGATRAN

Keisuke Mashima

JP2015503005A

June 13, 2018

February 27, 2014

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Takeda GmbH

C07D401/12; C07D213/71

JP2012501296A
JP2010520153A
JP2007513067A

WO2010098351A1
WO2003097603A1

Yasuyoshi ARIKAWA et al.,Discovery of a Novel Pyrrole Derivative 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-y,Journal of Medicinal Chemistry,2012年,Vol.55,p.4446-4456
YU Jing-hua et al.,Synthesis and Characterization of 2, 6-naphthalenedithiol,Journal of Beiging University of Chemical Technology,2005年,Vol.32, No.3,p.89-91

Takashima Ichi
Kyoko Doi
Mitsunori Kamata
Yaeko Tamura
Murata Miyuki
Junzo Koike
Hirofumi Toma

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