The a-L-rhamnopyranosyl phosphomonoesters conjugated with L-amino acid methyl esters were stereoselectively synthesized in a convenient route by utilizing H-phosphonate intermediate.
A convenient, efficient and general method has been developed for synthesis of H-phosphonate mono and diesters of AZT and d4T through one-pot reaction of phosphonic acid with AZT or d4T and different alcohols using pi...A convenient, efficient and general method has been developed for synthesis of H-phosphonate mono and diesters of AZT and d4T through one-pot reaction of phosphonic acid with AZT or d4T and different alcohols using pivaloyl chloride as condensing agent under mild conditions.展开更多
H-phosphonates were conveniently prepared by direct transesterification of diphenyl phosphite (DPP) with the corresponding alcohols, without further purification they were reacted with branched peptide methyl ester (L...H-phosphonates were conveniently prepared by direct transesterification of diphenyl phosphite (DPP) with the corresponding alcohols, without further purification they were reacted with branched peptide methyl ester (L-Leu2-L-LysOMe) through Atherton-Todd method, a series of different substituted alkyloxy (N-phosphoryl-L-Leu)2-L-LvsOMe were synthesized, and their structures were confirmed by P NMR, ESI-MS, H NMR,13 C NMR, IR and elemental analysis. 31 1 The approach possesses the advantages of easy operation, high yield and inexpensive phosphorylating reagent.展开更多
基金The authors would like to thank the financial supports from the NNSF of China(No.201 72033),the Ministry of Science and Technology,the Ministry of Education and Tsinghua University.
文摘The a-L-rhamnopyranosyl phosphomonoesters conjugated with L-amino acid methyl esters were stereoselectively synthesized in a convenient route by utilizing H-phosphonate intermediate.
基金Project supported by Excellent Dissertation Foundation by the Chinese Ministry of Education (No. 200222).
文摘A convenient, efficient and general method has been developed for synthesis of H-phosphonate mono and diesters of AZT and d4T through one-pot reaction of phosphonic acid with AZT or d4T and different alcohols using pivaloyl chloride as condensing agent under mild conditions.
基金The authors would like to thank the financial supports from the National Natural Science Foundation of China(No.20132020)the Ministry of Science and Technology.the Chinese Ministry of Education and Tsinghua University.
文摘H-phosphonates were conveniently prepared by direct transesterification of diphenyl phosphite (DPP) with the corresponding alcohols, without further purification they were reacted with branched peptide methyl ester (L-Leu2-L-LysOMe) through Atherton-Todd method, a series of different substituted alkyloxy (N-phosphoryl-L-Leu)2-L-LvsOMe were synthesized, and their structures were confirmed by P NMR, ESI-MS, H NMR,13 C NMR, IR and elemental analysis. 31 1 The approach possesses the advantages of easy operation, high yield and inexpensive phosphorylating reagent.
