An Efficient Synthesis of 3-Substituted <i>N</i>-Glycoside Indoles Useful as Sodium-Dependent Glucose Transporter Inhibitors
作者:Xun Li、Kenneth M. Wells、Shawn Branum、Sandra Damon、Scott Youells、Derek A. Beauchamp、David Palmer、Stephen Stefanick、Ronald K. Russell、William Murray
DOI:10.1021/op3001355
日期:2012.11.16
A practical synthesis of two N-glycoside indoles 1 and 2, identified as highly potent sodium-dependent glucose transporter (SGLT) inhibitors is described. Highlights of the synthetic process include a selective and quantitative Vilsmeier acylation and a high-yielding Grignard coupling reaction. The chemistry developed has been applied to prepare two separate SGLT inhibitors 1 and 2 for clinical evaluation
[EN] PROCESS FOR THE PREPARATION OF COMPOUNDS USEFUL AS INHIBITORS OF SGLT-2<br/>[FR] PROCÉDÉ DE PRÉPARATION DE COMPOSÉS UTILES À TITRE D'INHIBITEURS DE SGLT-2
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2012162115A3
公开(公告)日:2013-04-04
Shabarov, Yu. S.; Veselovskaya, S. V.; Saginova, L. G., Journal of Organic Chemistry USSR (English Translation), 1985, vol. 21, # 3, p. 481 - 484
作者:Shabarov, Yu. S.、Veselovskaya, S. V.、Saginova, L. G.
DOI:——
日期:——
Saginova, L. G.; Veselovskaya, S. V.; Shabarov, Yu. S., Journal of Organic Chemistry USSR (English Translation), 1984, vol. 20, # 6, p. 1106 - 1109
作者:Saginova, L. G.、Veselovskaya, S. V.、Shabarov, Yu. S.
DOI:——
日期:——
SAGINOVA, L. G.;VESELOVSKAYA, S. V.;SHABAROV, YU. S., ZH. ORGAN. XIMII, 1984, 20, N 6, 1216-1220
作者:SAGINOVA, L. G.、VESELOVSKAYA, S. V.、SHABAROV, YU. S.