[EN] INDAZOLE- AND PYRROLOPYRIDINE-DERIVATIVE AND PHARMACEUTICAL USE THEREOF<br/>[FR] DÉRIVÉ D'INDAZOLE ET PYRROLOPYRIDINE ET UTILISATION PHARMACEUTIQUE DE CELUI-CI
申请人:DAINIPPON SUMITOMO PHARMA CO
公开号:WO2012169649A1
公开(公告)日:2012-12-13
The present invention relates to a novel indazole- or pyrrolopyridine-derivative, represented by the formula (1) below, that has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same. Formula (1) [wherein each substituent is as defined in claim 1]
A simple catalyst of Ni(OAc)2 and P(t-Bu)3 enables selective C-alkylation of thioacetamides and primary acetamide with alcohols for the first time. Monoalkylation of thioamides, amides and t-butyl esters occurs in excellent yields (>95%). Mechanistic studies reveal that the reaction proceeds via a hydrogen autotransfer pathway.
Bromo Radical‐Mediated Photoredox Aldehyde Decarbonylation towards Transition‐Metal‐Free Hydroalkylation of Acrylamides at Room Temperature
作者:Zhaozhao Sun、Huawen Huang、Qiaolin Wang、Guo‐Jun Deng
DOI:10.1002/adsc.202101188
日期:2022.1.18
Herein, we report a visible-light-mediated hydroalkylation reaction of alkenes using easily available aldehydes as alkyl sources via bromo radical-promoted photoredox decarbonylation. This protocol provides an alternative entry to C(sp3)−C(sp3) bond formation and features considerable advantages including mild and clean reaction conditions, obviation for transition-metal catalyst, and good functional
作者:Hai T. Dao、Chao Li、Quentin Michaudel、Brad D. Maxwell、Phil S. Baran
DOI:10.1021/jacs.5b05144
日期:2015.7.1
problem of olefin hydromethylation is presented. This highly chemoselective method can tolerate labile and reactive chemical functionalities and uses a simple set of reagents. An array of olefins, including mono-, di-, and trisubstituted olefins, are all smoothly hydromethylated. This mild protocol can be used to simplify the synthesis of a specific target or to directly “edit” complex natural products
Thiophenol-Catalyzed Visible-Light Photoredox Decarboxylative Couplings of <i>N</i>-(Acetoxy)phthalimides
作者:Yunhe Jin、Haijun Yang、Hua Fu
DOI:10.1021/acs.orglett.6b03300
日期:2016.12.16
We have developed visible-light photoredox decarboxylative couplings of N-(acetoxy)phthalimides without an added photocatalyst in which simple and commercially available thiophenols are used as the effective organocatalysts, and 4-(trifluoromethyl)thiophenol shows optimal catalytic activity. Three representative decarboxylative examples were chosen including one amination and two C–C bond couplings