专利号:US-5442065-A 优先权日:1993-09-09 标 题:Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin 发明人:MAGNUS PHILIP D; ILIADIS THEODORE; EISENBEIS SHANE A; FAIRHURST ROBIN A 权利人:UNIV TEXAS 摘要:A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.
专利号:US-8779121-B2 优先权日:2012-10-12 标题:Process for the synthesis of 3-(2-bromo-4,5-dimethoxyphenyl)propanenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:US-7858828-B2 优先权日:2008-03-26 标 题 :Process for synthesis of (3R,3'R,6'R)-lutein and its stereoisomers 发明人:KHACHIK FREDERICK; CHANG AN-NI 权利人:UNIV MARYLAND 摘要:(3R,3′R,6′R)-Lutein and (3R,3′R)-zeaxanthin are two dietary carotenoids that are present in most fruits and vegetables commonly consumed in the US. These carotenoids accumulate in the human plasma, major organs, and ocular tissues. In the past decade, numerous epidemiological and experimental studies have shown that lutein and zeaxanthin play an important role in the prevention of age-related macular degeneration (AMD) that is the leading cause of blindness in the U.S. and Western World. The invention provides a process for the synthesis of (3R,3′R,6′R)-lutein and its stereoisomers from commercially available (rac)-α-ionone by a C 15 +C 10 +C 15 coupling strategy. In addition, the present invention also provides access to the precursors of optically active carotenoids with 3-hydroxy-ε-end group that are otherwise difficult to synthesize. The process developed for the synthesis of lutein and its stereoisomers is straightforward and has potential for commercialization.
专利号:US-7276637-B2 优先权日:2002-08-02 标题:Synthesis of cyclohexanone derivatives 发明人:BRANDS KAREL MARIE JOSEPH; DAVIES ANTONY JOHN; OAKLEY PAUL JOSEPH; SCOTT JEREMY PETER; SHAW DUNCAN EDWARD; TEALL MARTIN RICHARD 权利人:MERCK & CO INC 摘要:A novel process for preparing cyclohexanone derivatives of formula (I) n nis described. The products are useful as gamma secretase inhibitors, or as intermediates in the synthesis of other gamma secretase inhibitors.
专利号:US-4302612-A 优先权日:1976-07-15 标 题:Synthesis of perfluorodialdehydes 发明人:EVANS DAVID H; GREENWALD RICHARD B 权利人:POLAROID CORP 摘要:This invention is concerned with the synthesis of perfluorodialdehydes from the corresponding perfluorodiesters and with intermediates useful in the preparation of the perfluorodialdehydes.
专利号:US-8097720-B2 优先权日:2008-12-24 标题:Process for the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:PEGLION JEAN-LOUIS; DESSINGES AIMEE; SERKIZ BERNARD; LERESTIF JEAN-MICHEL; LECOUVE JEAN-PIERRE 权利人:PEGLION JEAN-LOUIS; DESSINGES AIMEE; SERKIZ BERNARD; LERESTIF JEAN-MICHEL; LECOUVE JEAN-PIERRE; LAB SERVER 摘要:Process for the synthesis of ivabradine of formula (I): n nand addition salts thereof with a pharmaceutically acceptable acid.
摘要:Abell, A. D.; Edmonds, M. K., Science of Synthesis, (2009) 46, 40. 摘要:Mase, N., Science of Synthesis Knowledge Updates, (2013) 3, 344. 参考文献:10.1134/s1068162008020179 摘要:Laptev AV, Belikov NE, Lukin AIu, Strokach IuP, Barachevskiĭ VA, Alfimov MV, Demina OV, Shvets VI, Skladnev DA, Khodonov AA. [Synthesis of spyropyran derivatives of retinal and study of their interaction with bacterioopsin from Halobacterium salinarum]. Bioorg Khim. 2008 Mar;34(2):276–84. doi: 10.1134/s1068162008020179.