Convenient synthesis of 1-aryl-9H-β-carboline-3-carbaldehydes and their transformation into dihydropyrimidinone derivatives by Biginelli reaction
作者： Péter Ábrányi-Balogh , András Dancsó , Dávid Frigyes , Balázs Volk , György Keglevich
DOI: 10.1016/J.TET.2014.06.073
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摘要: Abstract In the present work, a practical synthesis of 1-aryl-β-carboline-3-carbaldehydes as versatile building blocks and their application in Biginelli reaction is reported. The starting material four-step racemic tryptophan methyl ester. procedure involves Pictet–Spengler cyclization, dehydrogenation, an ester reduction, alcohol oxidation step. β-carboline-3-carbaldehydes were further transformed using into derivatives containing pharmacologically significant dihydropyrimidine ring at position-3.
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