专利号:US-5591854-A 优先权日:1994-10-14 标 题 :Enantioselective synthesis of seven-membered carbocycles and tropanes 发明人:DAVIES HUW M L 权利人:UNIV WAKE FOREST 摘要:A process of enantioselective synthesis of seven-membered carbocycles in the presence of di-rhodium(II) tetracarboxylate catalysts.
专利号:US-6486323-B1 优先权日:1998-09-30 标 题:Process for producing optically active tropinonemonocarboxylic acid derivative 发明人:NODE MANABU; NAKAMURA SOICHI; NAKAMURA DAISAKU 权利人:NIHON MEDIPHYSICS CO LTD 摘要:An optically active tropinonemonocarboxylic acid ester derivative useful as an intermediate for synthesis of optically active tropane derivatives was obtained by reacting succindialdehyde with an organic amine and acetonedicarboxylic acid ester to obtain a tropinonedicarboxylic acid ester derivative, and then subjecting this derivative to enzyme-catalyzed asymmetric dealkoxy-carbonylation. Since anhydroecgonine methyl ester derived from the optically active tropinone-monocarboxylic acid ester derivative by reduction and dehydration had the same direction of optical rotation as in the case of anhydroecgonine methyl ester obtained from natural cocaine, it was proved that the obtained optically active tropinonemonocarboxylic acid ester derivative had the same absolute configuration as that of natural cocaine. The yield of the optically active tropinonemonocarboxylic acid ester derivative from the asymmetric dealkoxycarbonylation was 30 to 50 mol %, and its optical purity was 70 to 97% ee. In addition, it was found that a crystalline optically active anhydroecgonine carboxylic acid ester derivative can be obtained by reducing and then dehydrating the optically active tropinonemonocarboxylic acid ester derivative and that its optical purity can easily be increased by recrystallization.
专利号:US-5736123-A 优先权日:1990-08-09 标 题 :Cocaine receptor binding ligands 发明人:CARROLL FRANK I 权利人:RES TRIANGLE INST 摘要:Novel compounds useful as intermediates in the synthesis of compounds having high affinity for specific cocaine receptors in the brain have the formula ##STR1## wherein R is (CH 2 ) n CH 2 Y, and wherein Y is H or F, X is a pharmaceutically acceptable anion, and n wherein Sn (R 1 , R 2 , R 3 ) is ortho, meta or para and wherein R 1 , R 2 , R 3 are independently alkyl of 1-6 carbon atoms and n is an integer of 0-5.
专利号:WO-9611928-A1 优先权日:1994-10-14 标 题:Enantioselective synthesis of seven-membered carbocycles and tropanes
专利号:EP-1238978-A2 优先权日:1999-05-12 标 题:Intermediates for the synthesis of radiolabelled tropanes
专利号:RU-2134264-C1 优先权日:1994-04-19 标题 :Derivatives of tropan-2-aldoxime, method of their synthesis, pharmaceutical composition and substances for drug production on said, method of treatment of patients with disorder or disease
参考文献:10.1002/(sici)1096-9888(199906)34:6<651::aid-jms817>3.0.co;2-m 摘要:Paul BD, McWhorter LK, Smith ML. Electron ionization mass fragmentometric detection of urinary ecgonidine, a hydrolytic product of methylecgonidine, as an indicator of smoking cocaine. J Mass Spectrom. 1999 Jun;34(6):651–60. doi: 10.1002/(sici)1096-9888(199906)34:6<651::aid-jms817>3.0.co;2-m. 参考文献:10.1520/jfs13254j 摘要:Ensing JG, Racamy C, de Zeeuw RA. A rapid gas chromatographic method for the fingerprinting of illicit cocaine samples. J Forensic Sci. 1992 Mar;37(2):446–59. 参考文献:10.1002/jms.310 摘要:Fandiño AS, Karas M, Toennes SW, Kauert G. Identification of anhydroecgonine methyl ester N-oxide, a new metabolite of anhydroecgonine methyl ester, using electrospray mass spectrometry. J Mass Spectrom. 2002 May;37(5):525–32. doi: 10.1002/jms.310.