专利号:US-2001044540-A1 优先权日:2000-03-23 标 题:Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors 发明人:PARSONS RODNEY L; DOROW ROBERTA L; DAVULCU AKIN H; FORTUNAK JOSEPH M; HARRIS GREGORY D; KAUFFMAN GOSS S; NUGENT WILLIAM A; RADESCA LILIAN A 摘要:This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.
专利号:US-6555686-B2 优先权日:2000-03-23 标题:Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors 发明人:PARSONS RODNEY L; DOROW ROBERTA L; DAVULCU AKIN H; FORTUNAK JOSEPH M; HARRIS GREGORY D; KAUFFMAN GOSS S; NUGENT WILLIAM A; RADESCA LILIAN A 权利人:BRISTOL MYERS SQUIBB PHARMA 摘要:This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.
专利号:US-8907104-B2 优先权日:2006-10-11 标 题 :Synthesis of enone intermediate 发明人:MYERS ANDREW G; BRUBAKER JASON D 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
专利号:US-8859765-B2 优先权日:2011-11-30 标 题:Process for the manufacture of chiral catalysts and their salts 发明人:WU PING-YU; HENSCHKE JULIAN PAUL 权利人:SCINOPHARM TAIWAN LTD 摘要:The present invention provides efficient and economical methods for synthesis of (−)-2-exo-morpholinoisoborne-10-thiol, its enantiomer, and related chiral catalysts. Novel compounds and methods of asymmetric synthesis are also disclosed.
专利号:US-8975427-B2 优先权日:2010-04-28 标题 :Synthesis of alkyl cyclopentadiene compounds 发明人:HARLAN C JEFF; CAO XIANYI; RIX FRANCIS C 权利人:HARLAN C JEFF; CAO XIANYI; RIX FRANCIS C; UNIVATION TECH LLC 摘要:A method of synthesizing an alkyl cyclopentadiene compound is disclosed. The method includes contacting at least one cyclopentadienyl anion source and at least one alkyl group source to form at least one alkyl cyclopentadiene compound. The method further includes extracting the alkyl cyclopentadiene compound with a hydrocarbon solvent. The alkyl cyclopentadiene compound may be converted to a metallocene catalyst compound.
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.
[参考文献]: An S, Et Al. Small-Molecule Protacs: An Emerging And Promising Approach For The Development Of Targeted Therapy Drugs. Ebiomedicine. 2018 Oct;36:553-562 [参考文献]: Ping-Yu Wu, Et Al. Asymmetric Synthesis Of Functionalized Diarylmethanols Catalyzed By A New Gamma-Amino Thiol. J Org Chem. 2006 Jan 20;71(2):833-5.
合成参考文献
参考文献:10.1007/s11046-006-0054-5 摘要:Bradshaw RE, Zhang S. Biosynthesis of dothistromin. Mycopathologia. 2006 Sep;162(3):201–13. doi: 10.1007/s11046-006-0054-5.