6-Chloro-2, 3, 4, 5-tetrahydro-3-methyl-1H-3-benzazepine: a potent and selective antagonist of. alpha. 2-adrenoceptors

RM DeMarinis, JP Hieble…

文献索引：DeMarinis, Robert M.; Hieble, J. Paul; Matthews, William D. Journal of Medicinal Chemistry, 1983 , vol. 26, # 9 p. 1213 - 1214

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被引用次数: 21

摘要

methylphenylacetamide (2) as a crystalline solid, mp 78-79" C (EtOAc). Reduction of amide 2 with diborane in THF yielded amino alcohol 3, in 93% yield as a colorless oil. Treatment of 3 in chloroform with phosphorous pentachloride in chloroform yielded 4, mp 115-117" C (EtOHEt20). This was cyclized at 175" C for 4 h in a melt of aluminum chloride and ammonium chloride to give 80%