A series of novel homochiral β-oligopeptides bearing aryl side chains was designed and synthesized from （S）-β-phenyl-β-amino acid derivatives by solution-phase methods. By means of circular dichroism（CD）, Fouri...A series of novel homochiral β-oligopeptides bearing aryl side chains was designed and synthesized from （S）-β-phenyl-β-amino acid derivatives by solution-phase methods. By means of circular dichroism（CD）, Fourier- transform infrared spectrometry（FTIR）, powder X-ray diffraction analysis（XRD） and density functional theory（DFT） calculations, we suggest that dipeptide P-2 and tripeptide P-3 adopt random coil-like conformations, pentapeptide P-5 and hexapeptide P-6 adopt stable 12-helix conformations in both solution and solid-state. Meanwhile, tetrapeptide P-4 adopt random coil-like conformation in solution and adopt 12-helix conformation in solid state.展开更多
A chiral Lewis base organocatalyzed enantioselective hydrosilylation ofa-keto ketimines was investigated.The reactions afforded various enantioenriched a-amino ketones with good yields（up to 95％） in moderate to goo...A chiral Lewis base organocatalyzed enantioselective hydrosilylation ofa-keto ketimines was investigated.The reactions afforded various enantioenriched a-amino ketones with good yields（up to 95％） in moderate to good enantioselectivities（up to 98％ e.e.）.Furthermore,one of the products was reduced to a chiral 1,2-amino alcohol.Following cyclization of it with triphosgene generated a cannabinoid receptor 1 （CB 1） inhibitor with good diastereoselectivity.展开更多
基金the National Natural Science Foundation of China（No.21172217）.
文摘A series of novel homochiral β-oligopeptides bearing aryl side chains was designed and synthesized from （S）-β-phenyl-β-amino acid derivatives by solution-phase methods. By means of circular dichroism（CD）, Fourier- transform infrared spectrometry（FTIR）, powder X-ray diffraction analysis（XRD） and density functional theory（DFT） calculations, we suggest that dipeptide P-2 and tripeptide P-3 adopt random coil-like conformations, pentapeptide P-5 and hexapeptide P-6 adopt stable 12-helix conformations in both solution and solid-state. Meanwhile, tetrapeptide P-4 adopt random coil-like conformation in solution and adopt 12-helix conformation in solid state.
基金Supported by the National Natural Science Foundation of China（No.20972155）.
文摘A chiral Lewis base organocatalyzed enantioselective hydrosilylation ofa-keto ketimines was investigated.The reactions afforded various enantioenriched a-amino ketones with good yields（up to 95％） in moderate to good enantioselectivities（up to 98％ e.e.）.Furthermore,one of the products was reduced to a chiral 1,2-amino alcohol.Following cyclization of it with triphosgene generated a cannabinoid receptor 1 （CB 1） inhibitor with good diastereoselectivity.
