专利号:US-5585252-A 优先权日:1988-08-30 标 题 :Enantio- and regioselective synthesis of organic compounds using enol esters as irreversible transacylation reagents 发明人:WONG CHI-HUEY; WANG YI-FONG; HENNEN WILIAM J 权利人:SEARLE & CO 摘要:A process for irreversible regio- and stereoselective enzyme catalyzed acylation of alcohols using enol esters as acylating reagents is disclosed. The present invention permits the selective modification of hydroxyl group(s) of chiral and meso alcohols, including sugars, organometallics, and glycosides. The enol freed upon transesterification rapidly tautomerizes to the corresponding volatile aldehyde or ketone thereby preventing the reverse reaction from occurring.
专利号:US-5106750-A 优先权日:1988-08-30 标 题:Enantio- and regioselective synthesis of organic compounds using enol esters as irreversible transacylation reagents 发明人:WONG CHI-HUEY; WANG YI-FONG; HENNEN WILLIAM J; BABIAK KEVIN A; DYGOS JOHN H; NG JOHN S 权利人:SEARLE & CO 摘要:A process for irreversible regio- and stereoselective enzyme catalyzed acylation of alcohols using enol esters as acylating reagents is disclosed. The present invention permits the selective modification of hydroxyl group(s) of chiral and meso alcohols, including sugars, organometallics, and glycosides. The enol freed upon transesterification rapidly tautomerizes to the corresponding volatile aldehyde or ketone thereby preventing the reverse reaction from occurring.
专利号:US-2005266068-A1 优先权日:2002-05-24 标题 :Cardiolipin molecules and methods of synthesis 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; AHMAD IMRAN 权利人:NEOPHARM INC 摘要:The invention provides new synthetic routes for cardiolipin with different fatty acids and/or alkyl chains with varying chain length and also with or without unsaturation, particularly a short-chain cardiolipin. The methods comprise reacting a 1,2-O-sn-diacyl/1,2-O-sn-dialkyl glycerol or a 2-O-protected glycerol, with a phosphoramidite reagent or a phosphate triester to produce a protected cardiolipin, which is deprotected to prepare the short chain cardiolipin. The reaction schemes can be used to generate new variants of cardiolipin. The cardiolipin prepared by the present methods can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs. Such liposomes can be used to treat diseases or in diagnostic and/or analytical assays. Liposomes can also include ligands for targeting a particular cell type or specific tissue.
专利号:WO-2004039817-A9 优先权日:2002-10-16 标题 :Cardiolipin molecules and method of synthesis 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; AHMAD IMRAN 权利人:NEOPHARM INC; AHMAD MOGHIS U; UKKALAM MURALI K; AHMAD IMRAN 摘要:The invention provides new synthetic routes for cardiolipin with different fatty acids and/or alkyl chains with varying chain length and also with or without unsaturation, particularly a short-chain cardiolipin. The methods comprise reacting a 1,2-O-sn-diacyl/1,2-O-sn-dialkyl glycerol or a 2-O-protected glycerol, with a phosphoramidite reagent or a phosphate triester to produce a protected cardiolipin, which is deprotected to prepare the short chain cardiolipin. The reaction schemes can be used to generate new variants of cardiolipin. The cardiolipin prepared by the present methods can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs. Such liposomes can be used to treat diseases or in diagnostic and/or analytical assays. Liposomes can also include ligands for targeting a particular cell type or specific tissue.
专利号:DE-68929190-T2 优先权日:1988-08-30 标 题:Enantio- and regioselective synthesis of organic compounds with enol esters as irreversible transacylation reagents
专利号:JP-2843606-B2 优先权日:1988-08-30 标题 :Enantio- and regio-selective synthesis of organic compounds using enol esters as irreversible acyl transfer reagents