专利号:US-8710210-B2 优先权日:2010-06-30 标题:Method of using N-thio compounds for oligonucleotide synthesis 发明人:HE YIGANG; SOROKIN VICTOR; MAZUR WIESLAW ADAM 权利人:HE YIGANG; SOROKIN VICTOR; MAZUR WIESLAW ADAM; GIRINDUS AMERICA INC 摘要:A method for synthesizing an oligonucleotide which comprises using a sulfurizing agent of general formula (I) for sulfurizing at least one phosphorus internucleotide linkage of a precursor of the oligonucleotide, wherein R is an aryl group or a heteroaryl group, which is bonded to the S-atom through an annular carbon atom; and R 1 and R 2 are independently organic residues, preferably a C1-C20 hydrocarbon residue. The method may further comprise purifying the oligonucleotide. Also included is a process for the synthesis of the sulfurizing agent.
专利号:US-8673885-B1 优先权日:2010-07-25 标 题 :Compounds for the protection of sulfur containing linkers in nucleic acid synthesis 发明人:DUFF ROBERT 权利人:DUFF ROBERT 摘要:Aromatic and alkyl thiocarbonates with and without a neighboring group that participates in the hydrolysis of a thiocarbonate are described. The aromatic or alkyl thiocarbonates can be used for the protection of sulfur during oligonucleotide synthesis. Their facile processes of manufacture and methods of using the same are provided.
专利号:US-2012071640-A1 优先权日:2008-12-23 标题 :Sulfurizing reagents and their use for oligonucleotides synthesis 发明人:MAZUR WIESLAW ADAM; HE YIGANG; SOROKIN VICTOR D 权利人:MAZUR WIESLAW ADAM; HE YIGANG; SOROKIN VICTOR D; GIRINDUS AMERICA INC 摘要:An oligonucleotide which comprises at least one internucleotide linkage comprising a P—S—R bond and at least two nucleosides, wherein R corresponds to the formula (I) n n n n n n n n n n wherein A is a geminally substituted alkylene group, preferably CH 2 , X and Y are independently selected from S and O, and R 0 is selected from the group consisting of optionally substituted carbon bonded organic residue, such as in particular optionally substituted alkyl or aryl, SRx, ORx and NRxRy wherein Rx and/or Ry are selected from H and organic residues and at least Rx is a substituent other than H. Another object of the invention is a sulfurizing agent useful for oligonucleotide manufacture and the manufacture thereof. Other nucleotides described comprise at least one internucleotide linkage comprising a P—S—R bond, at least one internucleotide linkage comprising a P—S—R′ bond and at least three nucleosides wherein R′ is an organic residue other than the group R, preferably selected from a group consisting of an aryl group and a heteroaryl group which is bonded to the S-atom through an annular carbon atom.
专利号:US-2014179875-A1 优先权日:2011-07-29 标题:Sulfurization reagents on solid supports 发明人:MAZUR WIESLAW ADAM; SOROKIN VICTOR; LAUGHLIN STEVEN KARL 权利人:MAZUR WIESLAW ADAM; SOROKIN VICTOR; LAUGHLIN STEVEN KARL; GIRINDUS AMERICA INC 摘要:Described herein are novel solid-supported sulfurization reagents having the general structure: (I) wherein (P) is a polymer; X is a linker; R 1 is an alkyl group, a cycloalkyl group, an aryl group, or a heterocycle; and R 2 is an alkyl group, an aryl group, a methyleneacyloxy group having the formula —CH 2 —O—C(O)—R 7 , a methylene carbonate group having the formula —CH 2 —O—C(O)—OR 8 , or a methylene carbamate group having the formula —CH 2 —O—C(O)—NR 9 R 10 , wherein R 7 is a C 1 to C 20 hydrocarbon residue, R 8 is any alkyl, cycloalkyl, aryl, or heteroaryl, and R 9 and R 10 are independently hydrogen, alkyl, cycloalkyl, aryl, or heteroaryl. Other embodiments include solid-supported sulfurization reagents having the structure of Formula I, wherein (P) is a polystyrene-based solid support and X is an aromatic linker. Also described herein are methods for synthesizing the solid-supported sulfurization reagents and their use during the synthesis of oligonucleotides.
专利号:WO-2010072831-A1 优先权日:2008-12-23 标题 :Sulfurizing reagents and their use for oligonucleotides synthesis 发明人:MAZUR WIESLAW ADAM; HE YIGANG; SOROKIN VICTOR 权利人:GIRINDUS AMERICA INC; MAZUR WIESLAW ADAM; HE YIGANG; SOROKIN VICTOR; GIRINDUS AG 摘要:An oligonucleotide which comprises at least one internucleotide linkage comprising a P-S-R bond and at least two nucleosides, wherein R corresponds to the formula (I) wherein A is a geminally substituted alkylene group, preferably CH 2 , X and Y are independently selected from S and O, and R 0 is selected from the group consisting of optionally substituted carbon bonded organic residue, such as in particular optionally substituted alkyl or aryl, SRx, ORx and NRxRy wherein Rx and/or Ry are selected from H and organic residues and at least Rx is a substituent other than H. Another object of the invention is a sulfurizing agent useful for oligonucleotide manufacture and the manufacture thereof.
专利号:US-2762836-A 优先权日:1952-12-08 标 题 :Synthesis of thiodinitriles 发明人:SELCER WILLIAM H 权利人:MONSANTO CHEMICALS
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