专利号:US-6800785-B1 优先权日:2002-10-15 标题:Process for the synthesis of estrogen receptor modulators 发明人:MENG DONGFANG 权利人:MERCK & CO INC 摘要:The present invention relates to processes for the synthesis of intermediates useful for the synthesis of estrogen receptor modulators. The process includes new methods for annelating 5-, 6- and 7-membered cycloalkenones onto an indanone.
专利号:US-7358382-B2 优先权日:2001-08-03 标 题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production of these new intermediate products in the synthesis and the use for the production of epothilones or epothilone derivatives.
专利号:US-7368568-B2 优先权日:2001-08-03 标 题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for production and the use 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroarnides for the synthesis of edothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
专利号:US-6933385-B2 优先权日:2001-08-03 标题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:SCHERING AG 摘要:The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
专利号:US-9403854-B2 优先权日:2001-03-30 标 题 :Cross-metathesis reaction of functionalized and substituted olefins using group 8 transition metal carbene complexes as metathesis catalysts 发明人:GRUBBS ROBERT H; CHATTERJEE ARNAB K; CHOI TAE-LIM; GOLDBERG STEVEN D; LOVE JENNIFER A; MORGAN JOHN P; SANDERS DANIEL P; SCHOLL MATTHIAS; TOSTE F DEAN; TRNKA TINA M 权利人:CALIFORNIA INST OF TECHN 摘要:The invention pertains to the use of Group 8 transition metal carbene complexes as catalysts for olefin cross-metathesis reactions. In particular, ruthenium and osmium alkylidene complexes substituted with an N-heterocyclic carbene ligand are used to catalyze cross-metathesis reactions to provide a variety of substituted and functionalized olefins, including phosphonate-substituted olefins, directly halogenated olefins, 1,1,2-trisubstituted olefins, and quaternary allylic olefins. The invention further provides a method for creating functional diversity using the aforementioned complexes to catalyze cross-metathesis reactions of a first olefinic reactant, which may or may not be substituted with a functional group, with each of a plurality of different olefinic reactants, which may or may not be substituted with functional groups, to give a plurality of structurally distinct olefinic products. The methodology of the invention is also useful in facilitating the stereoselective synthesis of 1,2-disubstituted olefins in the cis configuration.
专利号:US-6872727-B1 优先权日:1999-08-26 标 题:Polycyclic pyrimidine -2,4(1H,3H)-diones with functionalized alkyl residues at the 1- and/or 3-position(s); methods for their synthesis and pharmaceutical preparation 发明人:HERRMANN KONRAD; LEISTNER SIEGFRIED; WIPPICH PETRA 权利人:PRIVATES INST FUR BIOMEDIZINIS 摘要:Polycyclic pyrimidine-2,4(1H,3H)-diones with functionalized alkyl residues at the 1-, the 3-, or both position(s); methods for their synthesis, production, and pharmaceutical preparation. The invention concerns the synthesis of the above-described compounds, their chemical and structural characterization, and the analysis of their physiological/pharmacological activities in vitro and in vivo. These goals have been attained by the specification of routes of synthesis, methods for the production of the compounds, and the presentation of compound-specific characteristics. The substances encompassed by the present invention demonstrate pharmacologically significant collangenase/matrix metalloproteinase inhibitory activities. The specific example 1-(3-mercaptoprop-1-yl)-3-methyl-chinazolin-2,4(1H,3H)-dione will be presented in detail.
摘要:Diver, S. T., Science of Synthesis, (2009) 46, 130. 摘要:Michalak, M.; Gulajski, L.; Grela, K., Science of Synthesis, (2010) 47, 392. 摘要:Michalak, M.; Gulajski, L.; Grela, K., Science of Synthesis, (2010) 47, 354. 摘要:Bubnov, Yu. N.; Kolomnikova, G. D., Science of Synthesis Knowledge Updates, (2012) 3, 303. 摘要:Hashmi, A. S. K., Science of Synthesis Knowledge Updates, (2018) 1, 361.