Synthesis of Consecutive All-Carbon Quaternary Centers via Three-Step Reactions.

Consecutive all-carbon quaternary centers were synthesized in three steps from the corresponding ketones. The three reactions were (1) Knoevenagel condensation of ketone and malononitrile to afford dicyanoalkene, (2) 1,4-addition reaction of a Grignard reagent to dicyanoalkene, and (3) oxidative transformation of a malononitrile moiety to an ester, thioester, amide, and α-nitroketone. This method was applied to the synthesis of 17α-methyl steroids with a good yield and excellent diastereoselectivity.

Recent progress of sodium-glucose transporter 2 inhibitors as potential antidiabetic agents.

SGLT2 inhibitors were promising and novel antidiabetic drugs which suppressed glucose reabsorption and increased urinary glucose exertion. This review paper are aimed to summarize the recent progress of SGLT2 inhibitors during the last 5 years. This paper first summarizes the information of SGLT2 inhibitors, including mechanism, evolution and then focuses on the recent efforts on structure-activity relationships and structural optimization of SGLT2 inhibitors.