[EN] 2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS<br/>[FR] DÉRIVÉS DE 2,4-DIAMINOPYRIMIDINE EN TANT QU'INHIBITEURS DE PROTÉINE KINASES
申请人:AURIGENE DISCOVERY TECH LTD
公开号:WO2012059932A1
公开(公告)日:2012-05-10
The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.
Visible-light-promoted nitrone synthesis from nitrosoarenes under catalyst- and additive-free conditions
作者:Bao-Gui Cai、Lin Li、Guo-Yong Xu、Wen-Jing Xiao、Jun Xuan
DOI:10.1007/s43630-021-00062-6
日期:2021.6
A green and sustainable nitrone formation reaction via visible-light-promoted reaction of aryl diazoacetates with nitrosoarenes is described. This protocol exhibits good functional group tolerance and broad substrate scope for both aryl diazoacetates with nitrosoarenes. Comparing the reported methods for the synthesis of nitronesfrom nitrosoarenes, the reaction described herein occurs under sole visible-light
enantioselective hetero Diels-Alderreaction of a nitroso compound with a cyclic dienol, cyclohexa-l,3-dienylmethanol, has been realized utilizing stoichiometric amount of tartaric acidester as a chiralauxiliary to afford the corresponding dihydro-1,2-oxazine with complete regioselectivity and high enantioselectivity of up to 92% ee. A catalytic version of the asymmetric hetero Diels-Alderreaction of nitroso
利用化学计量的酒石酸酯作为手性助剂,实现了亚硝基化合物与环状二烯醇环己醇-1,3-二烯基甲醇的区域和对映选择性杂狄尔斯-阿尔德反应,得到相应的二氢-1,2 -恶嗪具有完全的区域选择性和高达 92% ee 的高对映选择性。还实现了亚硝基化合物与二烯醇的不对称杂 Diels-Alder 反应的催化形式,以提供高达 83% ee 的相应光学活性环加合物。添加 MS 4A 对于实现可重现的高对映选择性至关重要。
Tetrahydroquinolines via Stereospecific [3 + 3]-Annulation of Donor–Acceptor Cyclopropanes with Nitrosoarenes
作者:Saikat Das、Shyamal Chakrabarty、Constantin G. Daniliuc、Armido Studer
DOI:10.1021/acs.orglett.6b01302
日期:2016.6.3
A stereospecific [3 + 3]-annulation of donor–acceptorcyclopropanes with nitrosoarenes under the influence of MgBr2 as a stoichiometric Lewisacid and reagent offers a novel approach to various structurally diverse C-8-brominated tetrahydroquinolines. In these cascades C–C, C–N, and C–Br bonds are formed. The reactions are easy to conduct and proceed under mild conditions, and the products can readily
Multicomponent 1,3-Bifunctionalization of Donor–Acceptor Cyclopropanes with Arenes and Nitrosoarenes
作者:Saikat Das、Constantin G. Daniliuc、Armido Studer
DOI:10.1021/acs.orglett.6b02815
日期:2016.11.4
AlBr3-mediated multicomponent 1,3-bifunctionalization of donor–acceptor cyclopropanes using arenes and nitrosoarenes as coupling partners is presented. In the cascade, a C–C, a C–N, and a C–Br bond is formed. Reactions are easy to conduct and proceed under mild conditions. The γ,γ-disubstituted N-arylated α-amino esters obtained as products are readily further chemically modified rendering the method