专利号:US-9828340-B2 优先权日:2013-02-21 标题 :Asymmetric synthesis of a substituted pyrrolidine-2-carboxamide 发明人:FISHLOCK DANIEL; GU CHEN; SHU LIANHE; REGE PANKAJ DEVDATTA; SARMA KESHAB 权利人:HOFFMANN LA ROCHE 摘要:The invention relates to a process for the preparation of 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid of the formula (I) n nas well as intermediates thereof and pharmaceutical preparations thereof, comprising the step of reacting a compound of the formula (IV) with a compound of the formula (V), as defined in the specification, in the presence of a chiral silver- or copper catalyst.
专利号:WO-2014126954-A1 优先权日:2013-02-13 标题:Regioselective synthesis of substituted pyrimidines 发明人:CASTELHANO ARLINDO L; RECHKA JOSEF A; SENANAYAKE CHANDRAWANSHA; DEVANATHAN KRISHNASWAMY; GNANAVELU KARUNANIDHI 权利人:OSI PHARMACEUTICALS LLC 摘要:Disclosed are compounds of the Formula I:(I) where R 1 , R 4 , and R 5 are described herein, and methods of making the compounds, including regioselective functionalization.
专利号:WO-9729091-A1 优先权日:1996-02-09 标题:Balanol analogues 发明人:NIELSEN JOHN; LYNGSOE LARS OLE 权利人:AUDA PHARMACEUTICALS APS; NIELSEN JOHN; LYNGSOE LARS OLE 摘要:The present invention relates to a solid phase methodology for the preparation of a combinatorial library of structural analogues of the natural product balanol (ophiocordin, azepinostatin), which is a protein kinase C (PKC) and protein kinase A (PKA) inhibitor. The method comprises solid-phase synthesis of the analog variants of balanol whereby a high molecular diversity is introduced. The synthetic scheme is based on a retrosynthetic analysis of the native structure which revealed three main building blocks suitable as templates for modification. The dicarboxy-functional moiety can be immobilised to the polymer support either as the monoallyl ester or as the internal anhydride. The libraries produced by the method are especially suited for high throughput screening of potential drug candidates for the treatment of mammals, especially humans.
专利号:US-4118384-A 优先权日:1976-02-21 标题 :Process for preparation of azo dyestuffs by coupling in presence of aromatic sulphonic acid-formaldehyde reaction product 发明人:MOLLS HANS-HEINZ; SCHIWY WILLY; HORNLE REINHOLD; NEBELING REINHARD 权利人:BAYER AG 摘要:Dyestuff dispersions and dyestuff solutions free from salt or at least having a low salt content are obtained in that the diazotization is carried out with addition of free dispersing agent acid to which, after the synthesis, either no basic agents are added or basic agents are added only up to a pH value of 3. The disclosed process gives dyestuff compositions of low salt content and results in readily dispersible dyestuffs when water insoluble dyestuffs are prepared and stable solutions when water soluble dyestuffs are prepared. The process is widely applicable and chemical constitution of the dyestuffs is conventional.
专利号:US-4035350-A 优先权日:1975-01-30 标 题:Process for the preparation of water-soluble azo dyestuffs by reacting an aromatic amine and a coupling component with alkali metal nitrite or alkyl nitrite in the absence of acid 发明人:LANDLER JOSEF; WORFEL ERHARD 权利人:HOECHST AG 摘要:A new and very advantageous Process had been found for the preparation of azo dyestuffs by diazotation and coupling in which the synthesis is carried out without the hitherto usual addition of an acid, with the proviso that at least one of the diazo and coupling components contains at least one acid group. Besides the saving of reaction material and subsequently of alkali for neutralization of the reaction medium and isolation of the dyestuff, highly concentrated solutions of the dyestuff and salt-free or practically salt-free dyestuffs can be obtained, and waste-water is no longer charged with big amounts of salts.
专利号:US-2016002158-A1 优先权日:2013-02-21 标 题 :Asymmetric synthesis of a substituted pyrrolidine-2-carboxamide