The development of photoredox reactions of 1,3-dipolarcycloaddition of nitrones with alkenes is reported. It offers an efficient synthetic method to obtain isoxazolidine derivatives under mild conditions in synthetically useful yields. The nitrones are cyclized with oxidizable styrenes and aliphatic alkenes via a polar radical crossover cycloaddition reaction through photocatalytic reaction without
Visible photocatalysis of novel oxime phosphonates: synthesis of β-aminophosphonates
作者:Yong-Hong Li、Chun-Hai Wang、Su-Qian Gao、Feng-Ming Qi、Shang-Dong Yang
DOI:10.1039/c9cc06075h
日期:——
A novel type of oxime phosphonate was synthesized and used in the intermolecular cascade radical addition reaction of alkenes to access β-aminophosphonates via visible-light-driven N-centered iminyl radical-mediated and redox-neutral selective C–P single-bond cleavage in an active phosphorus radical route. The procedure is characterized by its ability to achieve the construction of Csp3–P and Csp3–N
[EN] KRAS G12D INHIBITORS<br/>[FR] INHIBITEURS DE KRAS G12D
申请人:MIRATI THERAPEUTICS INC
公开号:WO2021041671A1
公开(公告)日:2021-03-04
The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.
Visible-Light-Mediated Anti-Markovnikov Hydration of Olefins
作者:Xia Hu、Guoting Zhang、Faxiang Bu、Aiwen Lei
DOI:10.1021/acscatal.6b03388
日期:2017.2.3
avoided the need for a transition-metal catalyst, stoichiometric borane, as well as oxidant. Both terminal and internal olefins are readily accommodated in this transformation to obtain corresponding primary and secondary alcohols in good yields with single regioselectivity. This procedure can be scaled up to gram scale with a 230 turnover number based on photocatalyst.
A novel strategy involving visible-light-induced functionalization of alkenes for the synthesis of substituted aziridines was developed. The readily prepared N-protected 1-aminopyridinium salts were used for the generation of N-centered radicals. This approach allowed the synthesis of aziridines bearing various functional groups with excellent diastereoselectivity under mild conditions. Moreover, this