专利号:US-8901352-B2 优先权日:2011-01-13 标题 :Method for the synthesis of rasagiline 发明人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN 权利人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN; NOBEL ILAÇ SANAYII VE TICARET A S 摘要:We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.
专利号:US-6613910-B2 优先权日:2001-04-02 标题 :One-pot synthesis of group 8 transition metal carbene complexes useful as olefin metathesis catalysts 发明人:GRUBBS ROBERT H; MORGAN JOHN P; BENITEZ DIEGO; LOUIE JANIS 权利人:CALIFORNIA INST OF TECHN 摘要:The invention provides a novel method for synthesizing transition metal carbene complexes useful as olefin metathesis catalysts. The method is a convenient one-pot synthesis in which transition metal carbenes are prepared in high yield from readily available starting materials via a dihydrogen complex containing two different anionic ligands, preferably a phosphine and a heteroatom-stabilized carbene. The invention additionally provides a method for synthesizing precursors to carbene ligands useful, inter alia, in the aforementioned one-pot synthesis. The precursors are in the form of trichloromethyl adducts of the formula L 1 -CCl 3 , where L 1 is a heteroatom-stabilized carbene ligand, and are prepared by contacting an unsaturated, ionized analog of L-CCl 3 with a non-nucleophilic base in the presence of chloroform.
专利号:US-8809526-B2 优先权日:2010-07-19 标题 :Synthesis of cyclopentaquinazolines 发明人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; DALZIEL SEAN MARK; DAPREMONT Olivier; KIM HYUNJUNG; THOMPSON ANDREW S; ZELLER JAMES ROBERT 权利人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; DALZIEL SEAN MARK; DAPREMONT Olivier; KIM HYUNJUNG; THOMPSON ANDREW S; ZELLER JAMES ROBERT; ONYX PHARMA INC 摘要:A method of producing 6-amino-cyclopenta[g]quinazolines, in enantiomerically enriched form, is provided. In particular, the method may be applicable to the synthesis of N—{N-{4-[N-((6S)-2 -hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclo-penta[g]quinazolin-6-yl)-N-(prop-2 -ynyl)amino]benzoyl}-L-γ-glutamyl}-D-glutamic acid (ONX-0801).
专利号:US-4479859-A 优先权日:1983-12-27 标 题 :Laser photochemical synthesis of benzene and its derivatives 发明人:MCDONALD JOSEPH K; MERRITT JAMES A 权利人:US ARMY 摘要:A cw CO2 tunable laser is employed to irradiate an allyl halide selected from allyl chloride, allyl bromide, allyl fluoride, 2-methyl-3-chloropropene, and 2,3-dichloropropene and contained in one or more reaction cells at a predetermined pressure. A predetermined power level from about 25 to 150 watts, an irradiating time from about 0.2 second to about 60 seconds, and a selected radiation line for example P(36), P(32), P(28), P(26), or P(22) (that is resonant with an absorption band of the selected allyl halide) are employed to achieve dissociation of the selected allyl halide and to achieve a laser-induced photochemical synthesis of benzene and substituted benzenes.
专利号:US-4056573-A 优先权日:1975-04-24 标题:Synthesis of acyclic, terpene alcohols 发明人:CLOSE RALPH E; DERFER JOHN M 权利人:SCM CORP 摘要:Shown is a process for the synthesis of acyclic, terpene alcohols, such as 3,7-dimethyloctan-1-o1 and 7-substituted hydroxy or ethoxy derivatives thereof, wherein 3-methylbut-1-yn or the 3-substituted hydroxy or ether derivative thereof is coupled with a C5 coupling reagent having the configuration X being a leaving group such as chloride, bromide, iodide, tosylate and mesylate; R being or OR', R' being a lower alkyl up to 5 carbon atoms, phenyl, substituted phenyl up to 10 carbon atoms, cycloalkyl or aralkyl up to 10 carbon atoms, followed by hydrogenation and saponification or deetherification.
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.
摘要:Ohno, H.; Tomioka, K., Science of Synthesis, (2008) 44, 127. 摘要:Wang, K. K., Science of Synthesis, (2008) 44, 268. 摘要:Li, W.; Liu, X. H.; Feng, X. M., Science of Synthesis Knowledge Updates, (2021) 1, 29. 摘要:Delvos, L. B.; Oestreich, M., Science of Synthesis Knowledge Updates, (2017) 1, 149. 摘要:Okamoto, K.; Ohe, K., Science of Synthesis Knowledge Updates, (2020) 1, 67.