专利号:US-5623068-A 优先权日:1994-03-07 标 题:Synthesis of DNA using substituted phenylacetyl-protected nucleotides 发明人:REDDY M PARAMESWARA; FAROOQUI FIRDOUS; HANNA NAEEM B 权利人:BECKMAN INSTRUMENTS INC 摘要:Deoxyribonucleotide and ribonucleotide derivatives of the general formula I I wherein R1 represents -CR'R''-Ar, in which Ar is substituted aryl (as hereinafter defined) and R' and R'' are independently selected from the group consisting of hydrogen and lower alkyl; one of -R2 and R3 is a hydroxyl-protecting group and the other is a group suitable for synthesis of polynucleotides or for attachment of the nucleotide to a solid support; R4 is selected from the group consisting of hydrogen, -OH and protected hydroxyl; and B represents a divalent radical corresponding to a purine or pyrimidine base. When synthesis is carried out using these derivatives, the deprotection procedure is reduced to an essentially instantaneous process. The derivatives have acceptable shelf life and are very stable to conventional DNA synthesis conditions. Particularly preferred are those compounds wherein Ar is mono- and dihalo-substituted phenyl.
专利号:JP-H09510206-A 优先权日:1994-03-07 标 题 :Compositions and methods used in the synthesis of oligonucleotides
专利号:WO-9524413-A1 优先权日:1994-03-07 标 题 :Compositions and methods for use in the synthesis of oligonucleotides
专利号:EP-0749436-A1 优先权日:1994-03-07 标题:Compositions and methods for use in the synthesis of oligonucleotides
参考标题:Some Observations Relating To The Use Of 1-Aryl-4-Alkoxypiperidin-4-Yl Groups For The Protection Of The 2′-Hydroxy Functions In The Chemical Synthesis Of Oligoribonucleotides 作者:Wayne Lloyd,Colin B. Reese,Quanlai Song,Anthony M. Vandersteen,Cristina Visintin,Pei-Zhou Zhang 摘要:The Comparative Rates Of Acid-Catalysed Removal Of Ten 1-Aryl-4-Methoxypiperidin-4-Yl 8 (Râ =â Me) [including The Previously Reported Ctmp 5 And Fpmp 6] Protecting Groups For The 2A²-Hydroxy Functions In Oligoribonucleotide Synthesis Are Discussed. These Studies Have Led To The Development Of The 1-(4-Chlorophenyl)-4-Ethoxypiperidin-4-Yl (Cpep) Protecting Group 8 (Râ =â Et, R1A =â R2A =â H, R3A =â Cl) Which Is Both More Stable Than The Ctmp And Fpmp Groups At Ph 0.5 And More Labile At Ph 3.75. The Influence Of The Ribonucleoside Aglycone On The Stability Of The 2A²-O-Fpmp And 2A²-O-Ctmp Protecting Groups Both At Low And High Ph Is Examined.