| Literature DB >> 26871504 |
Yoshihito Ohtake1, Takashi Emura1, Masahiro Nishimoto1, Koji Takano1, Keisuke Yamamoto1, Satoshi Tsuchiya1, Sang-Yong Yeu1, Yasushi Kito2, Nobuaki Kimura3, Sunao Takeda3, Masao Tsukazaki2, Masatoshi Murakata3, Tsutomu Sato1.
Abstract
An efficient and scalable synthesis of an antidiabetic drug, tofogliflozin (1), which was identified as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor, is described. A key factor in the synthesis of 1 was the selection of the purpose-designed protecting group, which plays a strategic role in protection, chemoselective activation, and crystalline purification. The developed and optimized method made it possible to prepare 1 on a multidecagram scale without any column chromatography.Entities:
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Year: 2016 PMID： 26871504 DOI： 10.1021/acs.joc.5b02734
Source DB: PubMed Journal: J Org Chem ISSN： 0022-3263 Impact factor: 4.354