专利号:WO-2009030733-A1 优先权日:2007-09-04 标 题 :Method for the synthesis of 4-alkoxy-, 4-hydroxy- and 4-aryloxy-substituted tetrahydro-furo[3,4-b]furan-2(3h)-one compounds 发明人:QUAEDFLIEG PETER JAN LEONARD MARIO; ALSTERS PAULUS LAMBERTUS; STRAATMAN HENRICUS MARTINUS MARIO; HANBAUER MARTIN HELMUT FRIEDRICK 权利人:DSM IP ASSETS BV; QUAEDFLIEG PETER JAN LEONARD MARIO; ALSTERS PAULUS LAMBERTUS; STRAATMAN HENRICUS MARTINUS MARIA GERARDUS; HANBAUER MARTIN HELMUT FRIEDRI 摘要:The present invention relates to a method for the synthesis of enantiomerically and diastereomerically enriched 4-alkoxy-, 4-hydroxy- or 4-aryloxy- substituted tetrahydro-furo[3,4-b]furan-2(3H)-ones by aldol coupling of a suitable hydroxyl-protected hydroxy-acetaldehyde and 4-oxobutanoic acid or an ester thereof, and subsequent removal of the protecting group from the aldol compound and (optionally simultaneous) cyclizations and acetal formation under acidic conditions in the presence of an alcohol, followed by optional isolation of the desired compounds. The invention also relates to compounds according to formulae [Xl] and [XII].
专利号:US-8431745-B2 优先权日:2006-03-29 标题 :Process for preparation of HIV protease inhibitors 发明人:CRAWFORD KENNETH R; DOWDY ERIC D; GUTIERREZ ARNOLD; POLNIASZEK RICHARD P; YU RICHARD HUNG CHIU 权利人:CRAWFORD KENNETH R; DOWDY ERIC D; GUTIERREZ ARNOLD; POLNIASZEK RICHARD P; YU RICHARD HUNG CHIU; GILEAD SCIENCES INC 摘要:A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.
专利号:US-2010184989-A1 优先权日:2007-03-12 标 题 :De Novo Synthesis of Conjugates 发明人:RIGGS-SAUTHIER JENNIFER; DENG BO-LIANG; REN ZHONGXU; ZHANG WEN; GU XUYUAN; DUARTE FRANCO J 权利人:NEKTAR THERAPEUTICS 摘要:The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.
专利号:AU-2008226820-A1 优先权日:2007-03-12 标题 :De novo synthesis of conjugates
专利号:CA-2679473-A1 优先权日:2007-03-12 标题:De novo synthesis of conjugates
专利号:US-2010168422-A1 优先权日:2008-12-30 标 题:Methods and intermediates useful in the synthesis of hexahydrofuro [2,3-b]furan-3-ol 发明人:CHEN WEIPING 权利人:CHEN WEIPING 摘要:Provided herein are compounds and methods useful for preparing hexahydrofuro[2,3-b]furan-3-ol. Hexahydrofuro[2,3-b]furan-3-ol can be efficiently synthesized in four steps from readily available starting materials.
参考标题:Nonpeptidal P2 Ligands For Hiv Protease Inhibitors: Structure-Based Design, Synthesis, And Biological Evaluation 作者:Arun K. Ghosh,John F. Kincaid,D. Eric Walters,Yan Chen,Narayan C. Chaudhuri,Wayne J. Thompson,Chris Culberson,Paula M. D. Fitzgerald,Hee Yoon Lee,Sean P. Mckee,Peter M. Munson,Tien T. Duong,Paul L. Darke,Joan A. Zugay,William A. Schleif,Melinda G. Axel,Juinn Lin,Joel R. Huff |发布日期:1996.1.1 摘要:Design And Synthesis Of Nonpeptidal Bis-Tetrahydrofuran Ligands Based Upon The X-Ray Crystal Structure Of The Hiv-1 Protease-Inhibitor Complex 1 Led To Replacement Of Two Amide Bonds And A 10 Pi-Aromatic System Of Ro 31-8959 Class Of Hiv Protease Inhibitors. Detailed Structure-Activity Studies Have Now Established That The Position Of Ring Oxygens, Ring Size, And Stereochemistry Are All Crucial To