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Convenient Synthesis of 6-Bromo-1,2,3,4-tetrahydroisoquinoline and 3-Methoxy-1,2,3,4-tetrahydro-[2,7]-naphthyridine via Reductive Amination of Schiff's Bases
Authors:Pavol Zlatoidský  Bálint Gábos
Institution:1. AstraZeneca AB, Discovery Lund , Lund, Sweden Pavol.Zlatoidsky@astrazeneca.com;3. AstraZeneca AB, Discovery Lund , Lund, Sweden
Abstract:Synthesis of 7-bromo-1,2,3,4-tetrahydroisoquinoline and 6-methoxy-1,2,3,4-tetrahydro-2,7]-naphthyridine via lithiation of 2-methylarylidene-tert-butylamines, followed by formylation, reductive amination in one-pot, and removal of the tert-butyl group from the nitrogen, is described.
Keywords:Cyclization  formylation  lithiation  reductive amination
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