专利号:US-8530689-B2 优先权日:2008-05-05 标 题 :Processes for the preparation of biphenyl compounds 发明人:PERCEC VIRGIL; ROSEN BRAD MATTHEW; WILSON DANIELA A; WILSON CHRISTOPHER J 权利人:PERCEC VIRGIL; ROSEN BRAD MATTHEW; WILSON DANIELA A; WILSON CHRISTOPHER J; UNIV PENNSYLVANIA 摘要:The invention concerns processes for the synthesis of a compound of the formula: wherein: R 1 and R 2 are each, independently, C 1 -C 12 alkyl, CO 2 R 3 , OR 4 , R 5 (OR 6 ), or C 6 -C 18 aryl; R 3 -R 6 are each, independently, C 1 -C 12 alkyl or C 6 -C 12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising:—contacting a compound of the formula H0-R 7 -0H with BH 3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R 7 is a C 2 -C 12 hydrocarbon group and X is a halogen, OMs or OTs;—contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.
专利号:US-7884125-B2 优先权日:2008-04-30 标 题:Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues 发明人:STEVENS CHRISTIAN; HEUGEBAERT THOMAS 权利人:UNIV GENT 摘要:The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
专利号:US-6943194-B1 优先权日:1998-01-09 标题:Synthesis of phenstatin and prodrugs thereof 发明人:PETTIT GEORGE R; TOKI BRIAN 权利人:UNIV ARIZONA STATE 摘要:A newly discovered antineoplastic compound denominated “phenstatinâ€? is herein described as are synthetic methods for producing phenstatin and the active prodrug thereof. Phenstatin was converted to the sodium phosphate prodrug (3d) by a dibenzylphosphite phosphorylation and subsequent hydrogenolysis sequence 3b→3c→3d. Phenstatin (3b) was found to be a potent inhibitor of tubulin polymerization and the binding of colchicine to tubulin comparable to combretastatin A-4 (1b).
专利号:US-2009275616-A1 优先权日:2008-04-30 标 题 :Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues
专利号:WO-2024185814-A1 优先权日:2023-03-06 标题:Method for producing aryl compound containing tritylsulfanyl group 发明人:OKAZOE TAKASHI; NOZAKI KYOKO; GATZENMEIER Tim; LIU YUE 权利人:AGC INC; UNIV TOKYO 摘要:The present invention provides: a substrate for achieving the highly efficient synthesis of an aryl compound containing a tritylsulfanyl group; a method for producing a compound containing an SF 5 group using the substrate; and others. The present invention is a method for producing an aryl compound containing a tritylsulfanyl group, the method comprising thiotritylating a halogenated aryl compound represented by general formula (1) [wherein A 1 represents an aryl group that may have a substituent or a heteroaryl group that may have a substituent; and X represents a halogen atom] using [(triphenylmethyl)sulfanyl]potassium or [(triphenylmethyl)sulfanyl]sodium to produce an aryl compound containing a tritylsulfanyl group, the aryl compound being represented by general formula (2) [wherein A 1 is the same as A 1 in general formula (1); and Ph represents a phenyl group].
专利号:WO-9934788-A1 优先权日:1998-01-09 标 题:Synthesis of phenstatin and prodrugs thereof
摘要:Amatore, M.; Aubert, C.; Malacria, M.; Petit, M., Science of Synthesis Knowledge Updates, (2012) 3, 48. 摘要:Weibel, J.-M.; Blanc, A.; Pale, P., Science of Synthesis Knowledge Updates, (2018) 1, 42. 摘要:Chen, C.; Yu, L., Science of Synthesis Knowledge Updates, (2019) 3, 133. 摘要:Rudzinski, D. M.; Leadbeater, N. E., Science of Synthesis Knowledge Updates, (2012) 1, 373. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 22.