3-Amino-2-bromopyridine → HCID 10131088, compound

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Reaction Steps

tert-Butyl 3-[(2-bromo-3-pyridyl)carbamoyl]-1,2,5,6-tetrahydropyridine-1-carboxylate. 2-Bromo-3-pyridineamine (3.0 g, 17.3 mmol) and 1,2,5,6-tetrahydro-1,3-pyridinedicarboxylic acid 1-tert-butyl ester 3-methyl ester (5.05 g, 20.8 mmol) were dissolved in DCM (80 ml). To the solution trimethylaluminium (26 mmol, 2M solution) was slowly added at 0° C. The mixture was refluxed overnight. Work-up and purification on silica gel using 60% ethyl acetate in heptane as an eluent gave 5.65 g (85%) of the title compound.

Provenance & Evidence