作者:Chieh-Kai Chan、Yu-Lin Tsai、Yi-Ling Chan、Meng-Yang Chang
DOI:10.1021/acs.joc.6b01935
日期:2016.10.21
A new, four-step synthetic route for substituted 2,3-benzodiazepines 1, starting from aldehyde 4, was developed with excellent overall yields. This route included the 1,2-addition of various aromatic Grignard reagents to 4, PCC oxidation, and aerobic Wacker-type oxidation of the olefinic group of 6, followed by condensation of the resulting 1,5-dicarbonyl 7 with N2H4. Isoquinolones 9 were obtained
从醛4开始,开发了一种新的四步合成路线,用于取代2,3-苯并二氮杂1 1,具有极高的总收率。该途径包括将各种芳族格氏试剂1,2-加成4,PCC氧化和6的烯烃基的好氧Wacker型氧化,然后将所得的1,5-二羰基7与N 2 H 4缩合。。异喹诺酮9时来代替酮醛基获得。通过X射线单晶衍射分析确认了关键结构。