A robust and sustainable C(sp2)–C(sp3) cross-electrophile coupling was developed via nickel/copper synergistic catalysis under micellar conditions.
通过镍/铜协同催化在胶束条件下开发了稳健且可持续的C(sp²)–C(sp³)交叉电愿偶联。
Visible-Light-Initiated Manganese Catalysis for C−H Alkylation of Heteroarenes: Applications and Mechanistic Studies
作者:Philippe Nuhant、Martins S. Oderinde、Julien Genovino、Antoine Juneau、Yohann Gagné、Christophe Allais、Gary M. Chinigo、Chulho Choi、Neal W. Sach、Louise Bernier、Yvette M. Fobian、Mark W. Bundesmann、Bhagyashree Khunte、Mathieu Frenette、Olugbeminiyi O. Fadeyi
DOI:10.1002/anie.201707958
日期:2017.11.27
A visible‐light‐driven Minisci protocol that employs an inexpensive earth‐abundant metal catalyst, decacarbonyldimanganese Mn2(CO)10, to generate alkyl radicals fromalkyliodides has been developed. This Minisci protocol is compatible with a wide array of sensitive functional groups, including oxetanes, sugar moieties, azetidines, tert‐butyl carbamates (Boc‐group), cyclobutanes, and spirocycles. The
The identification of 8-ethyl-2-phenylamino-8H-pyrido[2, 3-d]pyrimidin-7-one (1) as an inhibitor of Cdk4 led to the initiation of a program to evaluate related pyrido[2, 3-d]pyrimidin-7-ones for inhibition of cyclin-dependentkinases (Cdks). Analysis of more than 60 analogues has identified some clear SAR trends that may be exploited in the design of more potent Cdk inhibitors. The most potent Cdk4
C–H Functionalization of Heteroarenes Using Unactivated Alkyl Halides through Visible-Light Photoredox Catalysis under Basic Conditions
作者:Noah B. Bissonnette、Michael J. Boyd、Gregory D. May、Simon Giroux、Philippe Nuhant
DOI:10.1021/acs.joc.8b01589
日期:2018.9.21
C–H functionalization of electron-deficient heteroarenes using commercial unactivated alkyl halides through reductive quenching photoredoxcatalysis was developed. Mainstream approaches rely on the use of an excess of strong acids that result in regioselectivities dictated by the innate effect of the protonated heteroarene, leaving the functionalization of other carbons unexplored. We report a mild
β-gem-dihalovinyl ketones/aldehydes with moderate to excellent yields in a highly regioselective manner. This reaction tolerates a wide scope of substrates, which offers a green and efficient entry to fabricate synthetically important β-gem-dihalovinyl carbonyl scaffolds. Notably, the late-stage application of these resulting β-gem-dihalovinyl carbonyls shows high and unique reactivity profiles and demonstrates