Compound 1 as a key intermediate of 1, 7, 9-trideoxytaxol was synthesized in ten steps from a biosynthetically available taxane, Sinenxan A. The key steps in the synthesis were deoxygenation at C-14, allylic oxidatio...Compound 1 as a key intermediate of 1, 7, 9-trideoxytaxol was synthesized in ten steps from a biosynthetically available taxane, Sinenxan A. The key steps in the synthesis were deoxygenation at C-14, allylic oxidation at C-13 and construction of the oxetane ring.展开更多
1-Hydroxyl acetylation of 10-deacetylbaccatin Ⅲ was achieved by removing the neighboring bulky 2-benzoyl group and oxidizing 2-hydroxyl group to a ketone function, but attempted reductive cleavage of 1-acetoxy gave r...1-Hydroxyl acetylation of 10-deacetylbaccatin Ⅲ was achieved by removing the neighboring bulky 2-benzoyl group and oxidizing 2-hydroxyl group to a ketone function, but attempted reductive cleavage of 1-acetoxy gave rearranged products under different conditions with or without proton source.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This research work was financially supported by NNSFC.
文摘Compound 1 as a key intermediate of 1, 7, 9-trideoxytaxol was synthesized in ten steps from a biosynthetically available taxane, Sinenxan A. The key steps in the synthesis were deoxygenation at C-14, allylic oxidation at C-13 and construction of the oxetane ring.
基金The authors gratefully acknowledge financial support from the National Natural Science Foundation of China(No.39370809)National New Drug Foundation(No.92-08-N).
文摘AF-5 was synthesized through a convergent method. The key step was the Robinson annulation using a key intermediate pentyl vinyl ketone.
文摘1-Hydroxyl acetylation of 10-deacetylbaccatin Ⅲ was achieved by removing the neighboring bulky 2-benzoyl group and oxidizing 2-hydroxyl group to a ketone function, but attempted reductive cleavage of 1-acetoxy gave rearranged products under different conditions with or without proton source.
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.
