专利号:US-2006009642-A1 优先权日:2001-10-12 标题 :Methods for the synthesis of substituted purines 发明人:DING SHENG; DING QIANG; GRAY NATHANAEL S; SCHULTZ PETER G 权利人:IRM LLC 摘要:The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines.
专利号:US-6949644-B2 优先权日:2001-10-12 标题 :Methods for the synthesis of substituted purines 发明人:DING SHENG; DING QIANG; GRAY NATHANAEL S; SCHULTZ PETER G 权利人:SCRIPPS RESEARCH INST 摘要:The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines. In one aspect, the present invention provides a method of preparing a 2,6,9-substituded purine compounds of Formula I: n n nthe method comprising:n a) oxidizing a resin-bound compound of Formula II: n n to provide a resin-bound compound of Formula III: n n b) reacting the compound of Formula III with an amine of Formula IVn nNR 3 R 4   IV,n nto provide a resin-bound compound of Formula V n n c) cleaving the resin-bound compound of Formula V from the resin to provide the substituted purine compounds of Formula I.
专利号:US-10533028-B2 优先权日:2014-09-04 标 题:Ruthenium complexes and their uses as catalysts in processes for formation and/or hydrogenation of esters, amides and related reactions 发明人:MILSTEIN DAVID; HU PENG; FOGLER ERAN; RAO JAI ANAND GARG NARAYANA 权利人:YEDA RES & DEV 摘要:The present invention relates to novel Ruthenium complexes of formulae A1-A4 and their use, inter alia, for (1) dehydrogenative coupling of alcohols to esters; (2) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (3) preparing amides from alcohols and amines—(including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or polymerization of amino alcohols and/or forming cyclic dipeptides from p-aminoalcohols; (4) hydrogenation of amides (including cyclic dipeptides, polypeptides and polyamides) to alcohols and amines; (5) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (6) dehydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e., synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water and a base to form carboxylic acids; and (10) preparation of amino acids or their salts by coupling of amino alcohols with water and a base. The present, invention further relates to the use of certain known Ruthenium complexes for the preparation of amino acids or their salts from amino alcohols.
专利号:US-8153817-B2 优先权日:2006-09-12 标 题 :Synthesis of methyl nonactate derivatives 发明人:BERGMEIER STEPHEN C; PRIESTLEY NIGEL D 权利人:BERGMEIER STEPHEN C; PRIESTLEY NIGEL D; UNIV OHIO 摘要:Methyl nonactate is converted into a variety of different triazoloamide antibacterial agents by a reaction scheme involving (1) inversion of the secondary alcohol of the methyl nonactate to produce the corresponding azidoester, (2) converting the azido ester to the corresponding azidoamide, and (3) converting the azido group of the azidoamide to a triazole to produce the corresponding triazoloamide.
专利号:US-7030230-B2 优先权日:2002-10-25 标题:Process of purifying phosphoramidites 发明人:ROSS BRUCE; SONG QUANLAI 权利人:ISIS PHARMACEUTICALS INC 摘要:A process of purifying phosphoramidite precursors useful in inter alia synthesis of oligonucleotides comprises dissolving a crude phosphoramidite in a polar phase, adding a basic compound to the polar phase, adding a portion of water to the polar phase, contacting the polar phase with a first apolar phase to extract impurity into the apolar phase, separating the first apolar phase from the polar phase, adding a second aliquot of water to the polar phase, and contacting the polar phase with a second apolar phase, whereby the phosphoramidite partitions into the second apolar phase.
专利号:US-12145139-B2 优先权日:2016-02-09 标题 :Manganese based complexes and uses thereof for homogeneous catalysis 发明人:MILSTEIN DAVID; NERUSH ALEX; VOGT MATTHIAS; MUKHERJEE ARUP; ESPINOSA-JALAPA NOEL ANGEL; CHAKRABORTY SUBRATA 权利人:YEDA RES & DEV; NERUSH ARKADI 摘要:The present invention relates to novel manganese complexes and their use, inter alia, for homogeneous catalysis in (1) the preparation of imine by dehydrogenative coupling of an alcohol and amine; (2) C—C coupling in Michael addition reaction using nitriles as Michael donors; (3) dehydrogenative coupling of alcohols to give esters and hydrogen gas (4) hydrogenation of esters to form alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (5) hydrogenation of amides (including cyclic dipeptides, lactams, diamide, polypeptides and polyamides) to alcohols and amines (or diamine); (6) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (7) dehydrogenation of secondary alcohols to ketones; (8) amidation of esters (i.e., synthesis of amides from esters and amines); (9) acylation of alcohols using esters; (10) coupling of alcohols with water and a base to form carboxylic acids; and (11) preparation of amino acids or their salts by coupling of amino alcohols with water and a base. (12) preparation of amides (including formamides, cyclic dipeptides, diamide, lactams, polypeptides and polyamides) by dehydrogenative coupling of alcohols and amines; (13) preparation of imides from diols.