- Regioselective Vinylation of Remote Unactivated C(sp3)?H Bonds: Access to Complex Fluoroalkylated Alkenes
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Regioselective incorporation of a particular functional group into aliphatic sites by direct activation of unreactive C?H bonds is of great synthetic value. Despite advances in radical-mediated functionalization of C(sp3)?H bonds by a hydrogen-atom transfer process, the site-selective vinylation of remote C(sp3)?H bonds still remains underexplored. Reported herein is a new protocol for the regioselective vinylation of unactivated C(sp3)?H bonds. The remote C(sp3)?H activation is promoted by a C-centered radical instead of the commonly used N and O radicals. The reaction possesses high product diversity and synthetic efficiency, furnishing a plethora of synthetically valuable E alkenes bearing tri-/di-/mono-fluoromethyl and perfluoroalkyl groups.
- Wu, Shuo,Wu, Xinxin,Wang, Dongping,Zhu, Chen
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supporting information
p. 1499 - 1503
(2019/01/04)
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- Synthesis of alkyne derivatives of a novel triazolopyrazine as A 2A adenosine receptor antagonists
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A novel [1,2,4]triazolo[1,5-a]pyrazine core was synthesized and coupled with terminal acetylenes. The structure-activity relationship of the alkynes from this novel template was studied for their in vitro and in vivo adenosine A2A receptor antagonism. Selected compounds from this series were shown to have potent in vitro and in vivo activities against adenosine A 2A receptor. Compound 12, in particular, was found to be orally active at 3 mg/kg in both a mouse catalepsy model and a 6-hydroxydopamine- lesioned rat model.
- Yao, Gang,Haque, Serajul,Sha, Li,Kumaravel, Gnanasambandam,Wang, Joy,Engber, Thomas M.,Whalley, Eric T.,Conlon, Patrick R.,Chang, Hexi,Kiesman, William F.,Petter, Russell C.
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p. 511 - 515
(2007/10/03)
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