Synthesis of aryl cyclopropyl sulfides through copper-promoted S-cyclopropylation of thiophenols using cyclopropylboronic acid
作者:Emeline Benoit、Ahmed Fnaiche、Alexandre Gagnon
DOI:10.3762/bjoc.15.113
日期:——
operates under simple conditions to afford the corresponding arylcyclopropyl sulfides in moderate to excellent yields. The reaction tolerates substitution in ortho-, meta- and para-substitution as well as electron-donating and electron-withdrawing groups. The S-cyclopropylation of a thiophenol was also accomplished using potassium cyclopropyl trifluoroborate.
First use of an organobismuth reagent in C(sp3)–S bond formation: Access to aryl cyclopropyl sulfides via copper-catalyzed S–Cyclopropylation of thiophenols using tricyclopropylbismuth
and operates under mild conditions to afford the corresponding aryl cyclopropyl sulfides in moderate to good yields. This reaction represents the first use of an organobismuth reagent in C(sp3)–S bondformation.
[Problem] To provide a compound which is useful as a GK activator.
[Means for Resolution] As a result of an extensive study on thiazole derivatives, the present inventors have found that a compound having an oxamoyl group, a glycol group or the like on a thiazole ring and a compound having an acetamide group substituted by a bicyclic heteroaryl group such as a quinolyl have a good GK activation effect, and thereby have accomplished the present invention.
Since the compounds of the present invention have a good GK activation effect, these are useful as therapeutic agents for diabetes, particularly type II diabetes.
Electrochemistry Enabled Nickel‐Catalyzed Selective C−S Bond Coupling Reaction
作者:Yang Wang、Feng Zhang、Yi Wang、Yi Pan
DOI:10.1002/ejoc.202101462
日期:2022.2.4
An electrochemically and catalytically regulated chemoselective C−Sbondcouplingreaction for the production of aryl sulfides and sulfones is reported.
报道了一种用于生产芳基硫化物和砜的电化学和催化调节的化学选择性 C-S 键偶联反应。
2-pyridone compounds
申请人:Kawaguchi Takanori
公开号:US08822503B2
公开(公告)日:2014-09-02
A 2-pyridone compound represented by the formula [1]:
wherein in the formula [1],
the ring represented by A represents a benzene ring or a pyridine ring,
X represents any of the structures represented by the formulas [3] shown below:
V represents a single bond or a lower alkylene group, and
W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)},
a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.