CAS: 2472-22-2; 6-Methoxy-3,4-Dihydronaphthalen-2(1H)-One

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6-甲氧基-3,4-二氢萘-1-基三氟甲磺酸酯置于dichloro(Cycloocta-1,5-Diene)Palladium (II),2-羟基-5-三氟甲基吡啶,水,C11H15No,Caesium Carbonate,2-二苯基磷-2'-(N,N-二甲氨基)联苯体系中,用 甲苯 用作溶剂,化学反应 35.0H,反应生成6-甲氧基-3,4-二氢-1H-2-萘酮
参考文献:Carbonyl 1,2-Transposition Through Triflate-Mediated α-Amination
标题:Carbonyl 1,2-Transposition Through Triflate-Mediated α-Amination
摘要:标题:酮转移的谨慎编排 化学家们致力于在分子框架中精确放置氧原子.吴等人报告了一种方便的方法,将羰基中的氧转移到相邻的碳中心.在将氧活化为烯基三氟乙酸酯后,钯和环辛烯的协同催化作用在邻近碳上加入氮,同时用氢化物取代三氟乙酸酯.然后水解产生所需的转移酮.该协议非常适合在药物优化期间对复杂分子进行后期变异.-jsy
Doi:10.1126/science.Abl7854

专利信息

专利号:RU-2014330-C1
优先权日:1988-05-23
标题:Method of synthesis of 1,2,3,4-tetrahydronaphthalene derivatives or their pharmaceutically acceptable acid-additive salt

专利号:US-8658806-B2
优先权日:2011-10-17
标 题:Process for preparing optically active antrocin
发明人：TAI DAR-FU; ANGAMUTHU VENKATACHALAM; TZENG YEW-MIN
权利人:TAI DAR-FU; ANGAMUTHU VENKATACHALAM; TZENG YEW-MIN; DEYEW BIOTECH CORP
摘要:The present invention relates to a process of preparation of optically active antrocin. At first, to introduce the correct configuration of trans-decalone, alkyl aluminum/TMSCN was used to react with decalenone. The resulting racemic nitrile-decalone was resolved with chiral diol by ketalization to produce two chromatography separable diasteromers. After a simple column chromatography, optically pure compounds were obtained. Formylation was a critical step for the lactone formation. The rest of the synthesis is straight forward through oxidation and olefination. Accordingly, the total synthesis was completed in 10 steps with 7% overall yield from commercially available 6-methoxy-2-tetralone.