Abstract

Pictet–Spengler condensation of β-arylethylamine with diethyl oxomalonate provides an entry to highly functionalized 1,1′-disubstituted tetrahydroisoquinoline in high yield. Selective functionalization of two ester groups is demonstrated. Syntheses and functional group transformations of 1,1-disubstituted tetrahydroisoquinoline are reported.

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