Dl-苯丙醇胺盐酸盐置于氢氧化钾,Sodium Hydroxide体系中,化学反应 6.67H,反应生成 (4R,5S)-(+)-4-甲基-5-苯基-2-恶唑啉酮 参考文献:Erythro-Directive Reduction Of .Alpha.-Substituted Alkanones By Means Of Hydrosilanes In Acidic Media 标题:Erythro-Directive Reduction Of .Alpha.-Substituted Alkanones By Means Of Hydrosilanes In Acidic Media 摘要: DOI:10.1021/jo00258A004
专利号:US-6603015-B2 优先权日:1999-03-29 标题:Synthesis of epothilones 发明人:GEORG GUNDA I; NAIR SAJIV K; REIFF EMILY; TUNOORI ASHOK RAO 权利人:UNIV KANSAS 摘要:Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.
专利号:US-6630602-B1 优先权日:1998-04-16 标题 :Propylisopropyl acetic acid and propylisopropyl acetamide stereoisomers, a method for their synthesis and pharmaceutical compositions containing them 发明人:BIALER MEIR; SPIGELSTEIN OFER; YAGEN BORIS 权利人:YISSUM RES DEV CO 摘要:The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines. The isomers are of the compound formula I:wherein R1 is a methyl or ethyl group; R2 is H, methyl or an ethyl group; R3 is ethyl or a propyl group; and R4 is a hydroxyl or amide group; and the total number of carbon atoms in said compound is 8, provided that when R1 is a methyl group and R4 is an amide group, R2 and R3 are not ethyl, further provided that when R1 is an ethyl and R4 a hydroxyl group, only stereoisomers of the compound are referred to. The present invention further relates to a method for the stereoselective synthesis of the 2S and 2R stereoisomer of PID and PIA. The present invention also relates to pharmaceutical compositions containing as an active ingredient a racemic mixture or stereoisomers of the compounds of the general formula (I), which are useful for the treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.
专利号:US-6969732-B2 优先权日:1999-04-12 标 题 :Propylisopropyl acetic acid and propylisopropyl acetamide stereoisomers, a method for their synthesis and pharmaceutical compositions containing them 发明人:BIALER MEIR; SPIGELSTEIN OFER; YAGEN BORIS 权利人:YISSUM RES DEV CO 摘要:The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines. The isomers are of the compound formula I n n R 1 is a methyl or ethyl group; R 2 is H, methyl or an ethyl group; R 3 is ethyl or a propyl group; and R 4 is a hydroxyl or amide group,n nand the total number of carbon atoms in said compound is 8, provided that when R1 is a methyl group and R4 is an amide group, R2 and R3 are not ethyl, further provided that when R1 is an ethyl and R4 a hydroxyl group, only stereoisomers of the compound are referred to.n nn The present invention further relates to a method for the stereoselective synthesis of the 2R stereoisomer of PID and PIA. The present invention also relates to pharmaceutical compositions containing as an active ingredient a racemic mixture or stereoisomers of the compounds of the general formula (I), which are useful for the treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.
专利号:US-6891059-B2 优先权日:2000-01-27 标题:Asymmetric synthesis of pregabalin 发明人:BURK MARK JOSEPH; GOEL OM PRAKASH; HOEKSTRA MARVIN SIMON; MICH THOMAS FREDERICK; MULHERN THOMAS; RAMSDEN JAMES A 权利人:WARNER LAMBERT CO 摘要:This invention provides a method of making (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid (pregabalin) or a salt thereof via an asymmetric hydrogenation synthesis. Pregabalin is useful for the treatment and prevention of seizure disorders, pain, and psychotic disorders. The invention also provides intermediates useful in the production of pregabalin.
专利号:US-6417399-B1 优先权日:1997-01-14 标 题:Amelioration of neurological disorders by the administration of (2R),(3S), and/or (2S),3(S) stereoisomers of valnoctamide 发明人:BIALER MEIR; YAGEN BORIS; SPIEGELSTEIN OFER; ROEDER MICHAEL; SCHURIG VOLKER 权利人:YISSUM RES DEV CO 摘要:The present invention generally relates to the individual stereoisomers of the drug valnoctamide (a mixture of four stereoisomer kinds, VCD-valmethamide or 2-ethyl-3-methyl pentanamide) useful in treatment of neurological and psychotic disorders such as different kinds of epilepsy and affective disorders, and useful as tranquilizers and to treat pain, and to pharmaceutical compositions containing, as an active ingredient, these stereoisomers. The present invention further relates to a method for stereoselective separation and quantification of the four stereoisomers from a racemic mixture of VCD or plasma of patients treated with the racemic drug. The present invention further relates to a unique method for the synthesis of the individual stereoisomers.
专利号:US-5561227-A 优先权日:1991-07-23 标题:Process for the stereospecific synthesis of azetidinones 发明人:THIRUVENGADAM TIRUVETTIPURAM K; TANN CHOU-HONG; MCALLISTER TIMOTHY L 权利人:SCHERING CORP 摘要:This invention provides an improved process for producing azetidinones. More particularly, this invention provides the steps of producing an azetidinone represented by the formula I ##STR1## from a carboxylic acid R 2 --D--CH 2 COOH, an aldehyde R 1 --A--CHO and an amine RNH 2 , by the steps of: (a) converting a carboxylic acid to the corresponding acid chloride; (b) deprotonating a chiral oxazolidinone and treating the resulting anion with the product of step (a); (c) enolizing the product of step (b) and condensing with an imine; and (d) cyclizing the product of step (c). Steps (c) and (d) of this process are as shown in the following reaction scheme. ##STR2##
参考标题:Synthetic Studies In The Lysocellin Family Of Polyether Antibiotics. The Total Synthesis Of Ferensimycin B 作者:David A. Evans,Richard P. Polniaszek,Keith M. Devries,Denise E. Guinn,David J. Mathre |发布日期:1991.9 摘要:A Convergent Asymmetric Synthesis Of The Polyether Antibiotic Ferensimycin B Has Been Completed. Chiral Enolate Bond Constructions Were Employed To Establish Seven Of The 16 Stereocenters Of The Subunits 35 And 52, Which Comprise The C& And Ci&3 Portions Of Ferensimycin B. The Stereogenic Centers At C3, C4, Cg, Clo, Ci6, C,,, And Cis Were Incorporated Through Internal Asymmetric Induction, While Those
合成参考文献
摘要:Banert, K., Science of Synthesis Knowledge Updates, (2015) 2, 278.