2,7-二羟基萘置于盐酸,Sodium Hydroxide,氨,Sodium体系中,用 乙醇,丙酮 作为反应溶剂,化学反应 0.5H,反应生成 7-甲氧基-2-萘满酮 参考文献:A Convenient Strategy For The Total Synthesis Of Pisiferic Acid Type Diterpenes 标题:A Convenient Strategy For The Total Synthesis Of Pisiferic Acid Type Diterpenes 摘要:A Practical Method For The Total Synthesis Of Pisiferic Acid Type Diterpenoids Is Described. This Involves Robinson Annulation Of The Keto Ester For The Key Intermediate. DOI:10.1081/scc-200046500
专利号:US-8932838-B2 优先权日:2010-06-17 标 题 :Biocatalysts and methods for the synthesis of (S)-3-(1-aminoethyl)-phenol 发明人:CABIROL FABIEN LOUIS; GOHEL ANUPAM; OH SEONG HO; SMITH DEREK J; WONG BRIAN; LALONDE JAMES J 权利人:CODEXIS INC 摘要:The present disclosure provides engineered transaminase polypeptides having improved properties as compared to naturally occurring transaminases including the ability of converting the substrate, 3′-hydroxyacetophenone to (S)-3-(1-aminoethyl)-phenol in enantiomeric excess and high percentage conversion. Also provided are polynucleotides encoding the engineered transaminases, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases to synthesize (S)-3-(1-aminoethyl)-phenol and related compounds useful in the production of active pharmaceutical ingredients.
专利号:US-8932836-B2 优先权日:2010-08-16 标 题:Biocatalysts and methods for the synthesis of (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine 发明人:LIMANTO JOHN; BEUTNER GREGORY; GRAU BRENDAN; JANEY JACOB; KLAPARS ARTIS; ASHLEY ERIC R; STROTMAN HALLENA R; TRUPPO MATTHEW D; HUGHES GREGORY; CABIROL FABIEN; GOHEL ANUPAM; COLLIER STEVEN J; LIANG JACK; MOCK MARISSA; MUNDORFF EMILY; NOVICK SCOTT; SMITH DEREK 权利人:LIMANTO JOHN; BEUTNER GREGORY; GRAU BRENDAN; JANEY JACOB; KLAPARS ARTIS; ASHLEY ERIC R; STROTMAN HALLENA R; TRUPPO MATTHEW D; HUGHES GREGORY; CABIROL FABIEN; GOHEL ANUPAM; COLLIER STEVEN J; LIANG JACK; MOCK MARISSA; MUNDORFF EMILY; NOVICK SCOTT; SMITH DEREK; CODEXIS INC 摘要:The disclosure provides transaminase polypeptides capable of converting the substrate, 2-(3,4-dimethoxyphenethoxy)cyclohexanone to the trans diastereomer product (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine in at least a 2:1 diastereomeric ratio relative to the cis diastereomer (1R,2S)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine. The disclosure also provides polynucleotides, vectors, host cells, and methods of making and using the transaminase polypeptides in processes for preparing (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine and its analogs, which can product compounds can be further used to prepare the aminocyclohexylether compound, (3R)-1-[(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]pyrrolidin-3-ol, which is an ion channel blocker.
专利号:US-9624478-B2 优先权日:2011-09-08 标题:Biocatalysts and methods for the synthesis of substituted lactams 发明人:CABIROL FABIEN LOUIS; CHEN HAIBIN; GOHEL ANUPAM; SALIM PAULINA ELENA; SMITH DEREK J; JANEY JACOB; KOSJEK BIRGIT; TANG WENG LIN; HSIEH HELEN; PHAM SON Q 权利人:CODEXIS INC 摘要:The present disclosure relates to transaminase polypeptides capable of aminating a dicarbonyl substrate, and polynucleotides, vectors, host cells, and methods of making and using the transaminase polypeptides.
专利号:US-4150032-A 优先权日:1978-01-18 标 题 :9-Oxobenzomorphan process and intermediates 发明人:KAVADIAS GERRY 权利人:BRISTOL MYERS CO 摘要:Improved processes for preparing 2'-alkoxy-2,5-di-substituted-9-oxo-6,7-benzomorphans from benz[e]indolines and synthesis of the benz[e]indoline intermediates are described. A representative example involves synthesis of 9b-allyl-8-methoxy-3-methyl-5,9b-dihydrobenz[e]indoline and bromination thereof to 9b-allyl-4-bromo-8-methoxy-2,4,5,9b-tetrahydro-1H-benz[e]indole methylbromide which is then hydrolyzed with a weak base such as ammonium bicarbonate to provide 5-allyl-2'-methoxy-2-methyl-9-oxo-6,7-benzomorphan.
专利号:US-4234731-A 优先权日:1979-01-05 标题:9-Oxobenzomorphan process 发明人:KAVADIAS GERRY 权利人:BRISTOL MYERS CO 摘要:Improved processes for preparing 2'-alkoxy-2,5-di-substituted-9-oxo-6,7-benzomorphans from benz[e]indolines and synthesis of the benz[e]indoline intermediates are described. A representative example involves synthesis of 9b-allyl-8-methoxy-3-methyl-5,9b-dihydrobenz[e]indoline and bromination thereof to 9b-allyl-4-bromo-8-methoxy-2,4,5,9b-tetrahydro-1H-benz[e]indole methylbromide which is then hydrolyzed with a weak base such as ammonium bicarbonate to provide 5-allyl-2'-methoxy-2-methyl-9-oxo-6,7-benzomorphan.
专利号:US-2017191043-A1 优先权日:2011-09-08 标题 :Biocatalysts and methods for the synthesis of substituted lactams
[参考文献]: J C Craig, Et Al. Synthesis And Dopaminergic Activity Of 2-Substituted Octahydrobenzo[f]Quinolines. J Med Chem. 1989 May;32(5):961-8.
合成参考文献
摘要:Simon, R. C.; Busto, E.; Fischereder, E.-M.; Fuchs, C. S.; Pressnitz, D.; Richter, N.; Kroutil, W., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 404. 摘要:Pandey, G.; Laha, R., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 160.