Imidazo-oxazaphosphorines as Precursors to Chiral Phosphite Triesters
摘要:
New bicyclic imidazo-oxazaphosphorines underwent a highly diastereoselective displacement of the imidazole moiety upon reaction with various alcohols, leading to chiral phosphite triesters as single diastereomers. The introduction of a nucleoside on this bicyclic structure was investigated by several routes, leading to new nucleoside building blocks.
Parasite glycoconjugates. Part 11.1 Preparation of phosphodisaccharide synthetic probes, substrate analogues for the elongating α-D-mannopyranosylphosphate transferase in the Leishmania
The present invention relates to a novel class of guanine nucleotide analogs which inhibit RelA and Relseq synthetic activity and which possess anti-bacterial activity. The present invention also relates to pharmaceutical compositions that include such compounds, and to methods of use of such compounds or compositions for combating bacteria and treating bacterial infections.
Tri(1-imidazolyl)phosphine (1) gave the cyclic phosphite quantitatively in the reactions with the diols possessing favorably placed hydroxyl groups in which the distance between the two oxygen atoms is 2.7–3.0 A. The both five- and six-membered cyclic phosphites were obtained quantitatively from the reactions of the diols possessing flexible chains with 1. The course of the selective formation of ribonucleoside
Synthesis of N6,N6-Dialkyladenine Nucleosides Using Hexaalkylphosphorus Triamides Produced in Situ
作者:Mahesh K. Lakshman、Asad Choudhury、Suyeal Bae、Eliezer Rochttis、Padmanava Pradhan、Amit Kumar
DOI:10.1002/ejoc.200800752
日期:——
Reactions between secondary amines and phosphorus trichloride (PCl3) leads to the formation of the corresponding tris(dialkylamino)phosphines or hexaalkylphosphorus triamides [HAPT: (R2N)3P]. Reaction of silyl-protected 2'-deoxyinosine and acetyl-protected inosine with the in situ formed HAPT and iodine (I2) leads to the formation of N6,N6-dialkyl adenosine and 2'-deoxyadenosine. In some cases the
Preparation of (2′-5′)-oligonucleotides based on 6-N-benzylaminopurineriboside using the Spicaria violacea fungal enzyme complex
作者:T. I. Kulak、O. V. Tkachenko、O. Yu. Grishan、T. A. Kukharskaya、L. A. Eroshevskaya、E. N. Kalinichenko、A. I. Zinchenko
DOI:10.1007/s10600-009-9249-6
日期:2009.1
A method for chemico-enzymatic synthesis of (2′-5′)-oligonucleotides with 6-N-benzylaminopurineriboside as the nucleoside units was proposed. The method consisted of enzymatic hydrolysis of the oligonucleotides with mixed (2′-5′)-(3′-5′)-phosphodiesterbonds that were prepared by polymerization of 6-N-benzyladenosine-2′(3′)-monophosphate by using (3′-5′)-specific nuclease and phosphatase contained in the filtrate of culture medium of the mycelial fungus Spicaria violacea.
Synthetic Fragments of Antigenic Lipophosphoglycans fromLeishmania major andLeishmania mexicana and Their Use for Characterisation of theLeishmania Elongating ?-D-Mannopyranosylphosphate Transferase
作者:Adrian P. Higson、Andrew J. Ross、Yury E. Tsvetkov、Fran�oise H. Routier、Olga V. Sizova、Michael A. J. Ferguson、Andrei V. Nikolaev
DOI:10.1002/chem.200400563
日期:2005.3.18
and 6, which are fragments of the phosphoglycan portion of the surface lipophosphoglycans from Leishmania mexicana (5) or L. major (6-9), were synthesised by using the glycosyl hydrogenphosphonate method for the preparation of phosphodiester bridges. The compounds were tested as acceptor substrates/putative inhibitors for the Leishmania elongating alpha-D-mannosylphosphate transferase.