三氟甲苯 反应生成 3-三氟甲基苯甲醛 参考文献:Hudlicky,M.,Collection Of Czechoslovak Chemical Communications,1960,Vol. 25,P. 1199-1209 标题:Hudlicky,M.,Collection Of Czechoslovak Chemical Communications,1960,Vol. 25,P. 1199-1209
专利号:US-6639059-B1 优先权日:1999-03-24 标 题 :Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.
专利号:US-6734291-B2 优先权日:1999-03-24 标题:Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs
专利号:US-6998484-B2 优先权日:2000-10-04 标 题:Synthesis of purine locked nucleic acid analogues 发明人:KOCH TROELS; JENSEN FLEMMING REISSIG 权利人:SANTARIS PHARMA AS 摘要:The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic substitution reaction of the 6-substituent in the purine ring and simultaneous nucleophile-induced intramolecular ring closure of the C-branched carbohydrate to form novel purine LNA analogues. The novel strategy is illustrated by the synthesis of the novel compound (1S,3R,4R,7S)-7-benzyloxy-1-methanesulfonylmethyl-3-(guanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane which is easily converted into (1S,3R,4R,7S)-7-hydroxy-1-hydroxymethyl-3-((2-N-isobutyrylguanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane after isobutyryl protection of the 2-amino purine group and subsequent substitution of 1-methanesulfonyl with benzoate, debenzoylation and debenzylation.
专利号:WO-2015109451-A1 优先权日:2014-01-22 标 题 :Synthesis of compounds containing 8-oxa-3-azabicyclo (3.2.1)octane ring 发明人:LI PENG; DECAMPO FLORYAN; SHI FENG; CUI XINJIANG; YUAN HANGKONG 权利人:RHODIA OPERATIONS; LANZHOU INSTITUTION OF CHEMICAL PHYSICS CHINESE ACADEMY OF SCIENCE 摘要:The present invention mainly pertains to catalytic processes for the direct amination of 2, -bis(hydroxymethyl) tetrahydrofuran to obtain compounds containing the 8-oxa-3-azabicyclo (3.2.1) octane ring, in the presence of: a homogenous catalyst which is a complex comprising at least one element selected from the group consisting of Iridium or Ruthenium and at least one donor ligand, or a heterogeneous catalyst comprising at least one Group 8-11 transition metal element and one poor metal element in the p-block of the period table.
专利号:US-8202985-B2 优先权日:2005-10-31 标 题:Monomer compositions for the synthesis of polynucleotides, methods of synthesis, and methods of deprotection 发明人:DELLINGER DOUGLAS J; TIMAR ZOLTAN; SIERZCHALA AGNIESZKA; DELLINGER GERALDINO; CARUTHERS MARVIN H 权利人:DELLINGER DOUGLAS J; TIMAR ZOLTAN; SIERZCHALA AGNIESZKA; DELLINGER GERALDINO; CARUTHERS MARVIN H; AGILENT TECHNOLOGIES INC; UNIV COLORADO 摘要:Nucleotide monomers, polynucleotides, methods of making each, and methods of deprotecting each, are disclosed. An embodiment of the nucleotide monomer, among others, includes a nucleotide monomer having a heterobase protecting group selected from structures I through III as described herein. An embodiment of the polynucleotide, among others, includes a plurality of nucleotide moieties having a heterobase protecting group selected from one of structures I through III as described herein.
专利号:US-7759471-B2 优先权日:2005-10-31 标题 :Monomer compositions for the synthesis of RNA, methods of synthesis, and methods of deprotection 发明人:DELLINGER DOUGLAS J; TIMAR ZOLTAN; SIERZCHALA AGNIESZKA; DELLINGER GERALDINE; CARUTHERS MARVIN H 权利人:AGILENT TECHNOLOGIES INC; UNIV COLORADO 摘要:Nucleotide monomers, polynucleotides, methods of making each, methods of deprotecting each, and the like are disclosed herein.