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Paper | Regular issue | Vol 89, No. 7, 2014, pp.1632-1643
Published online, 4th June, 2014
DOI: 10.3987/COM-14-13012
A Practical Synthesis of (4-(Spiro[chromane-2,4'-piperidin]-6-yl)phenyl)methanol as a Key Intermediate of Novel GPR119 Agonist

Tomoaki Koshizawa, Hayato Hosoi, Gen Watanabe, Toshiharu Morimoto, Tadaaki Ohgiya, and Kimiyuki Shibuya*

*Pharmaceutical Division, Tokyo New Drug Research Laboratories, Kowa Co., Ltd., 2-17-43, Noguchicho, Higashimurayama, Tokyo 189-0022, Japan

Abstract

Starting from commercially available 4'-hydroxy-[1,1'-biphenyl]- 4-carboxylic acid, a practical synthesis has been established in high yield for (4-(spiro[chromane-2,4'-piperidin]-6-yl)phenyl)methanol as a key intermediate for a novel GPR119 agonist.