专利号:US-8450365-B2 优先权日:2009-05-12 标 题 :Efficient synthesis of galanthamine 发明人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ 权利人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ; UNIV TEXAS 摘要:The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
专利号:US-7786156-B2 优先权日:2004-01-28 标 题 :Synthesis methods and intermediates for the manufacture of Rizatriptan 发明人:MARTIN PIERRE; BERENS ULRICH; BOUDIER ANDREAS; DOSENBACH OLIVER 权利人:RATIOPHARM GMBH 摘要:The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], n nor a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B]n n nwherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent.n n In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.
专利号:US-9090661-B2 优先权日:2009-03-27 标 题:Inhibitors of hepatitis C virus replication 发明人:COBURN CRAIG A; MCCAULEY JOHN A; LUDMERER STEVEN W; LIU KUN; VACCA JOSEPH P; WU HAO; HU BIN; SOLL RICHARD; SUN FEI; WANG XINGHAI; YAN MAN; ZHANG CHENGREN; ZHENG MINGWEI; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-3992392-A 优先权日:1973-04-27 标题:Synthesis of indoles from anilines and intermediates therein 发明人:GASSMAN PAUL G 权利人:UNIV OHIO STATE RES FOUND 摘要:Preparing indoles and intermediates therefor by reacting an N-haloaniline with a β-carbonylic hydrocarbon sulfide to form an azasulfonium halide, reacting the azasulfonium halide with a strong base to form a thio-ether indole derivative, and then reducing the thio-ether indole, e.g. with Raney nickel, to form the indole compound. When an acetal or ketal of the β-carbonyl hydrocarbon sulfide is used, the azasulfonium salt is treated with a base, and then with an acid to form the thio-ether indole derivative. When an α-ethyl-β -carbonylic hydrocarbon sulfide is used, the resulting azosulfonium salt reacts with strong base to form a thio-ether indolenine derivative, which on reduction with Raney nickel or complex metal hydrides yields 3-substituted indoles. The aniline may be an aminopyridine to form an aza-indole compound in the process. The azasulfonium salts and thio-ether indole or thio-ether indolenine derivatives can be isolated and recovered from their respective reaction mixtures. The thio-ether-indole and thio-ether indolenine derivatives are useful as intermediates to make the indoles without the thio-ether group. The indoles are known compounds having a wide variety of uses, e.g., in making perfumes, dyes, amino acids, pharmaceuticals, agricultural chemicals and the like.
专利号:US-9023813-B2 优先权日:2011-04-13 标题:Synthesis and use of glycoside derivatives of propofol 发明人:SHULL BRIAN; BALDWIN JOHN; GOPALASWAMY RAMESH; HAROON ZISHAN 权利人:SHULL BRIAN; BALDWIN JOHN; GOPALASWAMY RAMESH; HAROON ZISHAN; NUTEK PHARMA LTD 摘要:The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug propofol analogs. This invention relates to a method for the production of a broad group of glycosylated propofol carbohydrate derivatives.
专利号:US-9777013-B2 优先权日:2013-08-14 标题 :Derivatives of uncialamycin, methods of synthesis and their use as antitumor agents 发明人:NICOLAOU KYRIACOS C; LU MIN; MANDAL DEBASHIS; GANGWAR SANJEEV; CHOWDARI NAIDU S; POUDEL YAM B 权利人:UNIV RICE WILLIAM M; BRISTOL MYERS SQUIBB CO; SCRIPPS RESEARCH INST 摘要:In one aspect, the present disclosure provides new analogs of uncialamycin of formulae (I) and (II). The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates comprising the compounds of formulae (I) and (II).