During the synthesis of the derivatives of styryl ketonic Mannich bases, a side -product IM,other than the normal Mannich base MA, is obtained. Mannich reaction is further studied and the formation mechanism of produc...During the synthesis of the derivatives of styryl ketonic Mannich bases, a side -product IM,other than the normal Mannich base MA, is obtained. Mannich reaction is further studied and the formation mechanism of product IM is postulated and discussed on the basis of deuterium labelling.展开更多
Thirteen α-methylene aromatic araminenone and four α-methylene aromatic aminoketones were prepared by modified Mannich reaction. On the basis of isotopic labeling, a plausible way of cleavage was proposed for the fo...Thirteen α-methylene aromatic araminenone and four α-methylene aromatic aminoketones were prepared by modified Mannich reaction. On the basis of isotopic labeling, a plausible way of cleavage was proposed for the formation of the M^＋- 17 fragment peak in the MS of the α-methylene aromatic araminenone and aminoketones. The characteristic chemical shift of the olefinic protons in ^1H NMR is also discussed.展开更多
Fourteen substituted α-phenylcinnamic acids were prepared by the classical Perkin condensation. A plausible way of cleavage was involved in the formation of the specific fragment peaks in the MS of the α-phenylcinn...Fourteen substituted α-phenylcinnamic acids were prepared by the classical Perkin condensation. A plausible way of cleavage was involved in the formation of the specific fragment peaks in the MS of the α-phenylcinnamic acids . The characteristic chemical shift of the olefinic proton in HNMR is also discussed展开更多
Thirteen thiomorpholine-bearing compounds were designed and synthesized as dipeptidyl peptidase IV（DPP-IV） inhibitors, with natural and non-natural L-amino acids as the starting materials.Their structures were chara...Thirteen thiomorpholine-bearing compounds were designed and synthesized as dipeptidyl peptidase IV（DPP-IV） inhibitors, with natural and non-natural L-amino acids as the starting materials.Their structures were characterized by ~1H NMR,^（13）C NMR and HR-MS.The target compounds were screened for the DPP-IV inhibition,and the preliminary SAR result was obtained.Particularly, compounds 4c,4d and 4f with good DPP-IV inhibition in vitro were further evaluated through a mouse oral glucose tolerance test （OGTT）.The preliminary result showed the potential value for further studies on those thiomorpholine-bearing compounds as DPP-IV inhibitors.展开更多
基金the National Natural Science Foundation of China.
文摘During the synthesis of the derivatives of styryl ketonic Mannich bases, a side -product IM,other than the normal Mannich base MA, is obtained. Mannich reaction is further studied and the formation mechanism of product IM is postulated and discussed on the basis of deuterium labelling.
基金supported by the National Natural Science Foundation of China(No.39970867).
文摘Thirteen α-methylene aromatic araminenone and four α-methylene aromatic aminoketones were prepared by modified Mannich reaction. On the basis of isotopic labeling, a plausible way of cleavage was proposed for the formation of the M^＋- 17 fragment peak in the MS of the α-methylene aromatic araminenone and aminoketones. The characteristic chemical shift of the olefinic protons in ^1H NMR is also discussed.
文摘Fourteen substituted α-phenylcinnamic acids were prepared by the classical Perkin condensation. A plausible way of cleavage was involved in the formation of the specific fragment peaks in the MS of the α-phenylcinnamic acids . The characteristic chemical shift of the olefinic proton in HNMR is also discussed
基金the Fundamental Scientific Research Fund ofInstitute of Materia Medica(Li Peng 504-Basic 10 DPP IV inhibitor)for financial support on this project
文摘Thirteen thiomorpholine-bearing compounds were designed and synthesized as dipeptidyl peptidase IV（DPP-IV） inhibitors, with natural and non-natural L-amino acids as the starting materials.Their structures were characterized by ~1H NMR,^（13）C NMR and HR-MS.The target compounds were screened for the DPP-IV inhibition,and the preliminary SAR result was obtained.Particularly, compounds 4c,4d and 4f with good DPP-IV inhibition in vitro were further evaluated through a mouse oral glucose tolerance test （OGTT）.The preliminary result showed the potential value for further studies on those thiomorpholine-bearing compounds as DPP-IV inhibitors.
