Silica-Supported Polyphosphoric Acid in the Synthesis of 4-Substituted Tetrahydroisoquinoline Derivatives

作者: Stanimir Manolov , Stoyanka Nikolova , Iliyan Ivanov

DOI: 10.3390/MOLECULES18021869

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摘要: We report herein an application of α-amidoalkylation reaction, as alternative efficient synthesis 4-aryl- and 4-methyl-1,2,3,4-tetrahydroisoquinoline derivatives. The amides required for this purpose would result from reaction aminoacetaldehyde dimethylacetal with different substituted benzenes in polyphosphoric acid, followed by acylation the obtained amines acid chlorides or sulfochlorides. compared cyclisation step using conventional (milieu acetic-trifluoracetic = 4:1) solid supported reagents (SiO₂/PPA), recovered, regenerated reused without loss its activity catalyst. found that comparison to methods, yields are greater time is shorter.

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