Preparation of Synthetically Challenging Nucleotides Using Cyanoethyl P-Imidazolides and Microwaves
摘要:
We describe a general method for the elongation of nucleoside oligophosphate chains by means of cyanoethyl (CE) phosphorimidazolides. Though the method requires a phosphorylation and subsequent deprotection reaction, both steps could be achieved in one pot without isolation/purification of the initial phosphorylation product. We have also found that pyrophosphate bond formation by this method is significantly accelerated by microwave irradiation.
This paper describes the design and synthesis of a new type of aminoacyl-adenylate analogue (aa-AMPN) having an N-acyl phosphoramidate linkage where the oxygen atom of the mixed anhydride bond of aminoacyl-adenylate (aa-AMP) is replaced by an amino group. This new type of aa-AMP analogue is expected to be useful as material for studies on the recognition mechanism of the aminoacylation of tRNA and
[EN] 2'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES<br/>[FR] DÉRIVÉS DE NUCLÉOSIDE 2'-SUBSTITUÉS ET PROCÉDÉS D'UTILISATION DE CEUX-CI POUR LE TRAITEMENT DE MALADIES VIRALES
申请人:MERCK SHARP & DOHME
公开号:WO2012142085A1
公开(公告)日:2012-10-18
The present invention relates to 2'-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2'-Substituted Nucleoside Derivative, and methods of using the 2'-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
2'-AZIDO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
申请人:Girijavallabhan Vinay
公开号:US20140206640A1
公开(公告)日:2014-07-24
The present invention relates to 2′-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R
1
, R
2
and R
3
are as defined herein. The present invention also relates to compositions comprising at least one 2′-Azido Substituted Nucleoside Derivative, and methods of using the 2′-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
SOLID SUPPORTS AND PHOSPHORAMIDITE BUILDING BLOCKS FOR OLIGONUCLEOTIDE CONJUGATES
申请人:AM Chemicals LLC
公开号:US20180016232A1
公开(公告)日:2018-01-18
Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.
One-Pot Synthesis of Nucleoside 5′-Triphosphates from Nucleoside 5′-<i>H</i>-Phosphonates
作者:Qi Sun、Jocelyn P. Edathil、Runzhi Wu、Eric D. Smidansky、Craig E. Cameron、Blake R. Peterson
DOI:10.1021/ol8003029
日期:2008.5.1
Nucleoside5'-triphosphates (NTPs) play key roles in biology and medicine. However, these compounds are notoriously difficult to synthesize. We describe a one-pot method to prepare NTPs fromnucleoside5'-H-phosphonate monoesters via pyridinium phosphoramidates, and we used this approach to synthesize ATP, UTP, GTP, CTP, ribavirin-TP, and 6-methylpurine ribonucleoside-TP (6MePTP). Poliovirus RNA-dependent