专利号:US-10995049-B2 优先权日:2019-07-19 标 题 :Total synthesis of prostaglandin J natural products and their intermediates 发明人:LI JIAMING; XU CHEN; AHMED TONIA S; GRUBBS ROBERT H; STOLTZ BRIAN M 权利人:CALIFORNIA INST OF TECHN 摘要:The present disclosure is directed to methods of preparing prostaglandin J natural products by stereoretentive metatheses reactions and intermediates used in the synthesis of these natural products, including the use of intermediates of Formula (I-A), where R 1 is defined in the specification
专利号:US-4384127-A 优先权日:1981-04-08 标 题:Process for synthesis of optically pure prostaglandin E2 and analogs thereof 发明人:FUCHS PHILLIP L 权利人:PURDUE RESEARCH FOUNDATION 摘要:The invention comprises a multi-step synthesis of l(-) prostaglandin E 2 . The special features of the synthesis include: (1) a triply-convergent conjugate-addition and alkylation reaction involving the 1,4-addition of a chiral vinyl lithium reagent to a chiral vinylsulfone to produce a sulfone-stabilized anion. This anion is alkylated in situ to produce the basic prostaglandin skeleton structure, which is then subjected to (2) an efficient peracid oxidation of a secondary amine to a β-silyloxy oxime; and (3) an alkali-catalyzed 1,4-elimination of an α-sulfonyl oxime to produce a vinyl nitroso intermediate. This intermediate is treated with borohydride to give a stereospecific 1,4-reduction which yields the bis-silyloxy oxime of l(-)PGE 2 . Hydrolysis of the oxime, with concurrent cleavage of the silyloxy protecting groups, affords l(-)PGE 2 .
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-6765117-B2 优先权日:1997-10-24 标题:Process for stereoselective synthesis of prostacyclin derivatives 发明人:MORIARTY ROBERT M; PENMASTA RAJU; GUO LIANG; RAO MUNAGALA S; STASZEWSKI JAMES P 权利人:UNITED THERAPEUTIC CORP 摘要:An improved method is described for making 9-deoxy-PGF 1 -type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds. The invention also relates to novel intermediates prepared during the synthesis of the 9-deoxy-PGF 1 -type compounds.
专利号:US-2010159540-A1 优先权日:2007-03-26 标题:Synthesis of resolvins and intermediates, compounds prepared thereby, and uses thereof 发明人:RODRIGUEZ ANA; SPUR BERND 权利人:RODRIGUEZ ANA; SPUR BERND 摘要:Methods are disclosed for the preparation of a new class of lipid mediators known as resolvins, with Resolvin D6 (4,17-dihydroxy-5E,7Z,10Z,13Z,15E,19Z-docosahexaenoic acid) being exemplary. Also disclosed are methods for the efficient synthesis of key intermediates in the preparation of such resolvins, such as isotopically labeled ω-3 fatty acid metabolites, and derivatives and analogs thereof. The invention likewise extends to the intermediates so prepared, and to the resolvins prepared with their use.
专利号:US-9611206-B2 优先权日:2011-03-02 标题:Synthesis of intermediate for treprostinil production 发明人:SHARMA VIJAY 权利人:UNITED THERAPEUTICS CORP 摘要:The compound according to Formula I is an intermediate in the synthesis of prostacylin analogs. The present invention provides an efficient method for synthesizing a Formula I compound.
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