专利号:US-7202370-B2 优先权日:2003-10-27 标 题 :Semi-synthesis of taxane intermediates from 9-dihydro-13-acetylbaccatin III 发明人:NAIDU RAGINA 权利人:CONOR MEDSYSTEMS INC 摘要:A method is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel from 9-dihydro-13-acetylbaccatin III. The preparation of a suitably protected baccatin III backbone from 9-dihydro-13-acetylbaccatin III, and the insertion of the phenylisoserine side chain onto the protected baccatin III from 9-dihydro-13-acetylbaccatin III to form the taxane derivatives, paclitaxel and docetaxel is disclosed.
专利号:US-5498734-A 优先权日:1991-09-23 标 题:Preparation and use of (2-butene-1,4-diyl)magnesium complexes in organic synthesis 发明人:RIEKE REUBEN D 权利人:UNIV NEBRASKA 摘要:The magnesium complexes of cyclic hydrocarbons containing conjugated dienes, such as 1,2-dimethylenecycloalkanes, and 1,3-butadienes, are readily prepared in high yields using highly reactive magnesium. Reactions of these (2-butene-1,4 diyl)magnesium reagents with electrophiles such as dibromoalkanes, alkylditosylates, alkylditriflates, bromoalkylnitriles, esters, or amides serve as a convenient method for synthesizing carbocyclic systems. Significantly, carbocycles prepared by this method contain functional groups such as the exocyclic double bond or a keto group in one of the rings which could be used for further elaboration of these molecules. Furthermore, fused bicyclic systems containing a substituted five-membered ring can be conveniently prepared at high temperatures by the reactions of (2-butene-1,4-diyl)magnesium complexes with carboxylic esters or acid halides whereas low temperatures lead to regioselective synthesis of β,γ-unsaturated ketones. Additionally, γ-lactones, including spiro γ-lactones, can be easily prepared in a one pot synthesis from the reaction of (2-butene-1,4-diyl)magnesium complexes with a ketone or aldehyde and carbon dioxide. Also, δ-lactones can be easily prepared in a one pot synthesis from the reaction of (2-butene-1,4-diyl)magnesium complexes with epoxides followed by reaction with CO 2 . Use of α-hydroxy epoxides without the addition of CO 2 leads to the synthesis of vicinal diols. Chiral epoxides lead to chiral alcohols.
专利号:US-3681297-A 优先权日:1970-11-10 标 题 :Synthesis of polybenzothiazolines and polybenzothiazoles by reacting a dialdehyde with an aromatic bis-mercaptoamine 发明人:ALELIO GAETANO FRANCIS D 权利人:GAETANO FRANCIS D ALELIO 摘要:THIS INVENTION DEALS WITH A NOVEL, RELATIVELY SIMPLE PROCESS OF PREPARING POLYBENZOTHIAZOLINES, ((-NH-CH(-)-S-)>AR<(-NH-CH(-Z(-))-S-))N BY REACTING DIALDEHYDES, Z-(CH=O)2, AND (HS)2-AR(-NH2)2 IN A SOLVENT IN AN INERT ATMOSPHERE AND THEREAFTER OXIDIZING THE POLYBENZOTHIAZOLINES TO POLYBENZOTHIAZOLES, ((-N=C(-)-S-)>AR<(-N=C(-Z(-))-S-))N WHEREIN AR REPRESENTS A TETRAVALENT AROMATIC MOIETY IN WHICH THE NITROGEN AND SULFUR ATOMS IN EACH PAIR ARE DISPOSED ORTHO TO EACH OTHER AND Z REPRESENTS A DIVALENT HYDROCARBON MOIETY AS THE RESIDUE OF THE DIALDEHYDE, Z(CHO)2. NEW TYPES, AS WELL AS THE KNOW TYPES OF POLYBENZOTHIAZOLES HAVE BEEN PREPARED BY THIS PROCESS.
专利号:US-2007042401-A1 优先权日:2003-12-17 标题 :Methods for synthesis of encoded libraries
专利号:US-8815913-B2 优先权日:2006-12-06 标 题 :Metal-catalyzed copolymerization of imines and carbon monoxide as a route to synthesize polypeptides 发明人:SUN HUAILIN; ZHANG JIAN; LIU QIUHUA; YU LEI; ZHAO JIANGYU 权利人:SUN HUAILIN; ZHANG JIAN; LIU QIUHUA; YU LEI; ZHAO JIANGYU; UNIV NANKAI 摘要:Polypeptides of formula (I): n nwherein R 1 and R 2 are substituents independently selected from substituted and un-substituted alkyl groups and substituted and un-substituted aryl groups, and n is an integer greater than or equal to 2. Synthesis methods are also provided that do not use amino acids as starting materials, but instead employ imines and carbon monoxide as monomers that undergo transition metal-catalyzed alternating copolymerization to directly provide polypeptides using an acylcobalt catalyst with the following structural formula:n n nwherein R is selected from the group consisting of alkyl, phenyl, and substituted phenyl groups.
专利号:US-7972994-B2 优先权日:2003-12-17 标 题 :Methods for synthesis of encoded libraries