903566-45-0Relevant academic research and scientific papers
Development of a Scalable Synthesis of Tofogliflozin
Ohtake, Yoshihito,Emura, Takashi,Nishimoto, Masahiro,Takano, Koji,Yamamoto, Keisuke,Tsuchiya, Satoshi,Yeu, Sang-Yong,Kito, Yasushi,Kimura, Nobuaki,Takeda, Sunao,Tsukazaki, Masao,Murakata, Masatoshi,Sato, Tsutomu
, p. 2148 - 2153 (2016/03/15)
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.
Discovery of tofogliflozin, a novel C-arylglucoside with an O-spiroketal ring system, as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes
Ohtake, Yoshihito,Sato, Tsutomu,Kobayashi, Takamitsu,Nishimoto, Masahiro,Taka, Naoki,Takano, Koji,Yamamoto, Keisuke,Ohmori, Masayuki,Yamaguchi, Marina,Takami, Kyoko,Yeu, Sang-Yong,Ahn, Koo-Hyeon,Matsuoka, Hiroharu,Morikawa, Kazumi,Suzuki, Masayuki,Hagita, Hitoshi,Ozawa, Kazuharu,Yamaguchi, Koji,Kato, Motohiro,Ikeda, Sachiya
, p. 7828 - 7840 (2012/11/07)
Inhibition of sodium glucose cotransporter 2 (SGLT2) has been proposed as a novel therapeutic approach to treat type 2 diabetes. In our efforts to discover novel inhibitors of SGLT2, we first generated a 3D pharmacophore model based on the superposition o
SPIROKETAL DERIVATIVE AND USE THEREOF AS DIABETIC MEDICINE
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Page/Page column 21, (2008/06/13)
The present invention provides a compound of Formula (I): wherein R1, R2, R3 and R4 are each independently selected from a hydrogen atom, an optionally substituted C1-C6 alkyl group, an opt
