专利号:WO-0027627-A1 优先权日:1998-11-12 标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles 发明人:WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.
专利号:US-2006069270-A1 优先权日:2004-09-27 标 题 :Process for the preparation of 1,3,5-trisubstituted pyrazoles via [3+2] cycloaddition 发明人:SHAPIRO RAFAEL; ROSSANO LUCIUS T; TENHUISEN KAREN L 权利人:SHAPIRO RAFAEL; ROSSANO LUCIUS T; TENHUISEN KAREN L 摘要:A process for the preparation of 1,3,5-trisubstituted pyrazole compounds, which are useful intermediates in the synthesis of factor Xa inhibitors.
专利号:US-7153960-B2 优先权日:2001-12-10 标 题:Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones 发明人:ZHOU JIACHENG; OH LYNETTE M; MA PHILIP; LI HUI-YIN; CONFALONE PASQUALE 权利人:BRISTOL MYERS SQUIBB CO 摘要:A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. n nThese compounds are useful as factor Xa inhibitors.
专利号:US-4822903-A 优先权日:1981-05-15 标题:Fluorinated silica catalyst and preparation of aromatic/aliphatic nitriles in the presence thereof 发明人:JACQUES ROLAND; REPPELIN MICHEL; SEIGNEURIN LAURENT 权利人:RHONE POULENC SPEC CHIM 摘要:An improved fluorinated siliceous catalyst, well adapted for the catalytic synthesis of aromatic/aliphatic nitriles from their corresponding formamides, formanilides or amides, is comprised of a plurality of silica particulates, the specific surface of which ranging from about 200 to about 300 m 2 /g, having a total pore volume ranging from about 1 to about 1.5 cm 3 /g, with an average pore diameter ranging from about 100 to about 200 â„«, having an exchange pH of less than about 3, and with the fluorine content thereof bonded to the silica, expressed in F 31 , ranging from about 0.05 to about 2% by weight based upon the silica, and the sodium content thereof, expressed as Na 2 O, being less than about 1% by weight, also based upon the silica.
专利号:WO-9731891-A1 优先权日:1996-03-01 标 题:Process for regioselective substitution of trifluorobenzoate or trifluorobenzonitrile 发明人:LYNCH JOSEPH E; SHI YAO-JUN; WELLS KENNETH M 权利人:MERCK & CO INC; LYNCH JOSEPH E; SHI YAO JUN; WELLS KENNETH M 摘要:The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.
专利号:US-2025313551-A1 优先权日:2022-12-15 标题 :Process for the preparation of a quinazolinone derivative 发明人:DOTT PASCAL JEAN CLAUDE; FANTASIA SERENA MARIA; GUILLEMOT-PLASS MAUD; KALDRE DAINIS; LARI GIACOMO MARCO; MODOLO-CHELLAT ISABELLE GEORGETTE HUGUETTE; SEDELMEIER JOERG MATHIAS; TROKOWSKI SEBASTIAN 权利人:HOFFMANN LA ROCHE 摘要:The present invention relates to a new process for the preparation of (3R)—N-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide, as well as to a novel intermediate useful for the synthesis of said compound at large scale.
[参考文献]: Haopeng Wang, Et Al. High-Sensitivity Elemental Ionization For Quantitative Detection Of Halogenated Compounds. Analyst. 2015 Dec 21;140(24):8177-85. [参考文献]: S D Lepore, Et Al. Studies On The Synthetic Compatibility Of Aryloxime Linkers In The Solid-Phase Synthesis Of 3-Aminobenzisoxazoles. J Org Chem. 2000 May 19;65(10):2924-32. [参考文献]: S Thomas, Et Al. Aminoborohydrides. 12. Novel Tandem S(N)Ar Amination-Reduction Reactions Of 2-Halobenzonitriles With Lithium N,N-Dialkylaminoborohydrides. J Org Chem. 2001 Mar 23;66(6):1999-2004.
合成参考文献
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