专利号:US-7705159-B2 优先权日:2005-07-06 标题:Process for the preparation of letrozole 发明人:MACDONALD PETER LINDSAY; BIGATTI ETTORE; ROSSETTO PIERLUIGI; HAREL ZVI 权利人:SICOR INC 摘要:The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.
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:US-7816375-B2 优先权日:2000-09-11 标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
专利号:US-4369322-A 优先权日:1978-12-15 标 题 :Process for the production of substituted acetonitriles 发明人:SCHALKE PETER; KLEEMANN AXEL 权利人:DEGUSSA 摘要:The known synthesis for the production of aromatic substituted acetonitriles by reaction of aromatic substances with cyanogen chloride in the gas phase is improved by feeding the starting materials in gaseous form and separated from each other into the reactor. The process can be used to synthesize in general aromatic and especially hetero-aromatic substituted acetonitrile.
专利号:US-3714159-A 优先权日:1971-03-30 标 题:2,2-diaryl-4-(4'-aryl-4'-hydroxy-piper-idino)-butyramides 发明人:JANSSEN P; NIEMEGEERS C; STOKBROEKX R; VANDENBERK J 权利人:JANSSEN PHARMACEUTICA NV 摘要:COMPOUNDS OF THE CLASS OF 2,2-DIARYL-4-(4''-ARYL-4''HYDROXY-PIPERIDINO)BUTYRAMIDES WHEREIN SAID ARYL AND SAID AMIDE FUNCTIONS ARE VARIOUSLY DEFINED GROUPS, SAID BUTURAMIDES HAVING ANTI-DIARRHEAL AND ANALGESIC ACTVITES; ALSO INCLUDED ARE NOVEL INTERMEDIATES USED IN THE SYNTHESIS OF SAID BUTYRAMIDES.
专利号:WO-2007104696-A1 优先权日:2006-03-15 标题 :Antimalarial agents having polyaromatic structure 发明人:CAMPIANI GIUSEPPE; GEMMA SANDRA; FATTORUSSO CATERINA; KUKREJA GAGAN; JOSHI BHUPENDRA PRASAD; TAGLIALATELA SCAFATI ORAZIO; SAVINI LUISA; DE ANGELIS MERI; FATTORUSSO ERNESTO 权利人:SIGMA TAU IND FARMACEUTI; CAMPIANI GIUSEPPE; GEMMA SANDRA; FATTORUSSO CATERINA; KUKREJA GAGAN; JOSHI BHUPENDRA PRASAD; TAGLIALATELA SCAFATI ORAZIO; SAVINI LUISA; DE ANGELIS MERI; FATTORUSSO ERNESTO 摘要:Antimalarial agents having a novel pharmacophore of formula (I) are herein described. These polycyclic compounds are able to inhibit chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum (Pf). Furthermore, the synthesis of these compounds involves few steps from commercial products with low cost of production.
[参考文献]: Julieta Rangel De Oliveira, Et Al. Biotransformation Of Phenylacetonitrile To 2-Hydroxyphenylacetic Acid By Marine Fungi. Mar Biotechnol (Ny). 2013 Feb;15(1):97-103.
合成参考文献
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