专利号:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
专利号:US-9938509-B2 优先权日:2010-12-08 标 题 :Biocatalysts and methods for the synthesis of armodafinil 发明人:ANG EE LUI; ALVIZO OSCAR; BEHROUZIAN BEHNAZ; CLAY MICHAEL D; COLLIER STEVEN J; EBERHARD ELLEN D; FAN FU; SONG SHIWEI; SMITH DEREK J; WIDEGREN MAGNUS; WILSON ROBERT; XU JUNYE; ZHU JUN 权利人:CODEXIS INC 摘要:The present invention relates to non-naturally occurring polypeptides useful for preparing armodafinil, polynucleotides encoding the polypeptides, and methods of using the polypeptides. The non-naturally occurring polypeptides of the present invention are effective in carrying out biocatalytic conversion of the (i) 2-(benzhydrylsulfinyl)acetamide to (−)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide (armodafinil), or (ii) benzhydryl-thioacetic acid to (R)-2-(benzhydrylsulfinyl)acetic acid, which is a pivotal intermediate in the synthesis of armodafinil, in enantiomeric excess.
专利号:US-4937367-A 优先权日:1987-07-15 标 题:Process for the preparation of intermediates for the synthesis of fosfomycin 发明人:CASTALDI GRAZIANO; GIORDANO CLAUDIO 权利人:ZAMBON SPA 摘要:A process is described for the preparation of intermediates useful in the synthesis of Fosfomycin. n More particularly, an enantioselective process is described for the preparation of derivatives of (1S,2S)-1,2-dihydroxypropyl-phosphonic acid of formula ##STR1## wherein R 2 and R 3 have the meanings reported in the specification.
专利号:WO-03050105-A2 优先权日:2001-12-10 标题 :Catalytic asymmetric synthesis of optically active compounds 发明人:HALLAND NIS; JOERGENSEN KARL ANKER; HANSEN TORE 权利人:CHEMINOVA AS; HALLAND NIS; JOERGENSEN KARL ANKER; HANSEN TORE 摘要:A one step catalytic asymmetric process for the synthesis of an optically active compound of formula la or lb wherein R is selected from C1-7 alkyl, C1-7 haloalkyl, C1-7 alkoxy, C1-7 haloalkoxy, halogen and hydroxy; R3 is H or C1-4 alkyl; R4 is selected from H, C1-7 alkyl, C1-7 haloalkyl, C1-7 alkoxy, COOH, CO-C1-7 alkoxy and an optionally substituted aryl or heterocycle; AR represents C1-7 alkyl, optionally substituted aryl, an optionally substituted heterocycle or AR and R4 may be bridged together forming part of a ring system; X is O or S; m is a number between 0-4; comprising the step of reacting a compound of the formula 2 with a compound of formula 3 in the presence of a catalytic amount of a chiral nitrogen containing organic compound.
专利号:US-4101557-A 优先权日:1966-09-23 标题:Selective synthesis of 2-haloalkanethiols and episulfides therefrom 发明人:MUELLER WOLFGANG H; OSWALD ALEXIS A; KOZAK PETER J 权利人:EXXON RESEARCH ENGINEERING CO 摘要:Haloalkanethiols are synthesized through the free radical liquid phase reaction of halogenated olefins with an excess of hydrogen sulfide. High product yields to the desired haloalkanethiol products are secured when a 3 to 20 fold molar excess of hydrogen sulfide to halogenated olefin is used. Desirably, the synthesis is carried out to a conversion level not exceeding 90%. The haloalkanethiol products can be subsequently dehydrohalogenated to the corresponding episulfide products by reacting the haloalkanethiol product with a substantially equal molar amount of anhydrous ammonia.
专利号:US-6867202-B1 优先权日:1997-06-25 标 题 :Treatment of insulin resistance 发明人:CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL 权利人:PFIZER 摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
参考标题:Heterogeneously Catalyzed Direct Ch Thiolation Of Heteroarenes 作者:Suhelen Vásquez-Céspedes,Angélique Ferry,Lisa Candish,Frank Glorius |发布日期:2015.5.4 摘要:The First General Methodology For The Direct Thiolation Of Electron‐rich Heteroarenes Was Developed By Employing Pd/al2O3, A Recoverable And Commercially Available Heterogeneous Catalyst, And Cucl2. This Method Represents An Operationally Simple Approach For The Synthesis Of These Valuable Compounds. Preliminary Mechanistic Studies Indicate A Heterogeneous Catalytic System, In Which Both Metals Play
合成参考文献
摘要:Schatz, J.; Seler, M., Science of Synthesis Knowledge Updates, (2011) 2, 433. 摘要:Schatz, J.; Seler, M., Science of Synthesis Knowledge Updates, (2011) 2, 385. 摘要:Schatz, J.; Seler, M., Science of Synthesis Knowledge Updates, (2011) 2, 406. 摘要:Schatz, J.; Seler, M., Science of Synthesis Knowledge Updates, (2011) 2, 404. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 22.