专利号:US-5760237-A 优先权日:1995-08-25 标 题 :Synthesis of l-azatyrosine using pseudoephedrine as a chiral auxiliary 发明人:MYERS ANDREW G 权利人:CALIFORNIA INST OF TECHN 摘要:A practical synthesis of the potential chemotherapeutic agent L-azatyrosine is described. The key step involved the alkylation of (R,R)-(-)-pseudoephedrine glycinamide with 5-benzenesulfonyloxy-2-iodomethylpyridine and proceeded in 70-95% yield and 89-95% de. Simultaneous hydrolysis of the auxiliary and the benzenesulfonate protecting group afforded L-azatyrosine of ≧99% ee in 73% yield on multigram scale (recovery yield of (R,R)-(-)-pseudoephedrine: 90%).
专利号:US-8664402-B2 优先权日:2011-03-09 标题:Process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone, an intermediate of etoricoxib 发明人:CASTELLIN ANDREA; STABILE PAOLO; FONTANA FRANCESCO; DE LUCCHI OTTORINO; CAPORALE ANDREA; TARTAGGIA STEFANO 权利人:CASTELLIN ANDREA; STABILE PAOLO; FONTANA FRANCESCO; DE LUCCHI OTTORINO; CAPORALE ANDREA; TARTAGGIA STEFANO; ITALIANA SINT SPA 摘要:A process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methyl sulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. The synthesis of the intermediates useful for such preparation is also described.
专利号:RU-2024511-C1 优先权日:1986-04-17 标 题 :Method of synthesis of e-isomers of acrylic acid derivatives
专利号:US-9670230-B2 优先权日:2012-11-29 标题 :Heteroaryl compounds and methods of use thereof 发明人:CAMPBELL JOHN EMMERSON; JONES PHILIP 权利人:SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
专利号:US-6936600-B2 优先权日:1999-04-01 标题:Sorbitol dehrydrogenase inhibitors 发明人:CHU-MOYER MARGARET Y; MYLARI BANAVARA L; ZEMBROWSKI WILLIAM J 权利人:PFIZER 摘要:This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, n n nwherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.
专利号:US-5998451-A 优先权日:1987-10-19 标 题 :Substituted tetralins, chromans and related compounds in the treatment and related compounds in the treatment of asthma, arthritis and related diseases 发明人:EGGLER JAMES F; MARFAT ANTHONY; MELVIN JR LAWRENCE S 权利人:PFIZER 摘要:Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.
[参考文献]: Margaret E Welk, Et Al. Out-Of-Center Distortions In D(0) Transition Metal Oxide Fluoride Anions. Inorg Chem. 2002 Oct 7;41(20):5119-25.
合成参考文献
摘要:Giel, M.-C.; Smedley, C. J.; Moses, J. E., Science of Synthesis, (2021) , 442. 摘要:Schafer, E. W., Jr., and W. A. Bowles Jr. 1985. Acute oral toxicity and repellency of 933 chemicals to house and deer mice. Archives of Environmental Contamination and Toxicology 14:111-129. https://www.aphis.usda.gov/ws/nwrc/chem-effects-db/S_schafer851.pdf