N,N-Dimethyl-1,3-propanediamine → tert-Butyl 4-(2-(3-(Dimethylamino)propylamino)quinazolin-4-ylamino)piperidine-1-carboxylate

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Reaction Steps

tert-Butyl 4-(2-chloroquinazolin-4-ylamino)piperidine-1-carboxylate (3.34 g. 9.21 mmol) and 3-(N,N-dimethyl amino)propylamine (2.9 ml, 23.03 mmol) in dioxane (15 ml) in a sealed-tube were heated to 120° C. overnight. The solvent was removed and the crude product was purified by silica gel column chromatography using 10% NH3 ca. 7 N MeOH in CH2Cl2 and 90% CH2Cl2 solution as eluent to produce the title compound as a pure white solid.

Provenance & Evidence