A facile catalytic enantioselective 1,2-addition of diynes to trifluoromethyl ketones was developed. By a com- bination of Me2Zn, Ti(OPr-i)4, BaF2 and quinine, the reaction of a series of terminal diynes with triflu...A facile catalytic enantioselective 1,2-addition of diynes to trifluoromethyl ketones was developed. By a com- bination of Me2Zn, Ti(OPr-i)4, BaF2 and quinine, the reaction of a series of terminal diynes with trifluoromethyl ke- tones proceeded to afford trifluoromethylated chrial tertiary alcohols with the diyne moiety in good to high yields with moderate to high enantioselectivities. Furthermore, this catalytic asymmetric diyne addition to trifluoro- methylketone was applied in the synthesis of the Efavirenz analogue.展开更多
Simple and readily available chiral N-(sulfinyl)allylamines have been developed as efficient novel ligands for the rhodium-catalyzed enantioselective 1,2-addition of arylboronic acids to challenging aliphatic a-keto...Simple and readily available chiral N-(sulfinyl)allylamines have been developed as efficient novel ligands for the rhodium-catalyzed enantioselective 1,2-addition of arylboronic acids to challenging aliphatic a-ketoesters. By employing the linear or branched sulfinamide-olefin ligands, interesting enantioselectivity as well as regioselectiw ity reversal in the related asymmetric additions were observed.展开更多
A series of homoallyl β', γ'-unsaturated amines were synthesized via1,2-addition of α,β-unsaturated imines with allylsamarium bromide in excellent yields under mildand neutral conditions.
文摘A facile catalytic enantioselective 1,2-addition of diynes to trifluoromethyl ketones was developed. By a com- bination of Me2Zn, Ti(OPr-i)4, BaF2 and quinine, the reaction of a series of terminal diynes with trifluoromethyl ke- tones proceeded to afford trifluoromethylated chrial tertiary alcohols with the diyne moiety in good to high yields with moderate to high enantioselectivities. Furthermore, this catalytic asymmetric diyne addition to trifluoro- methylketone was applied in the synthesis of the Efavirenz analogue.
基金Financial support from the National Natural Science Foundation of China
文摘Simple and readily available chiral N-(sulfinyl)allylamines have been developed as efficient novel ligands for the rhodium-catalyzed enantioselective 1,2-addition of arylboronic acids to challenging aliphatic a-ketoesters. By employing the linear or branched sulfinamide-olefin ligands, interesting enantioselectivity as well as regioselectiw ity reversal in the related asymmetric additions were observed.
基金theNationalNaturalScienceFoundationofChina (No .2 0 0 72 0 33)andNaturalScienceFoundationofZhejiangProvince ,China
文摘A series of homoallyl β', γ'-unsaturated amines were synthesized via1,2-addition of α,β-unsaturated imines with allylsamarium bromide in excellent yields under mildand neutral conditions.