Triethylamine → Tert-butyl 4-(6-fluoroquinazolin-2-yl)-6,7-dimethyl-1,4-diazepane-1-carboxylate

Participants

Reaction Conditions

Reaction Steps

The amine 1-4 (270 mg, 1.18 mmol) was combined with 2-chloro-6-fluoroquinazoline 1-8 (216 mg, 1.18 mmol; see example 1-D), and triethylamine (412 uL, 2.96 mmol), in DMF (5 mL) and heated to 130° C. for 3 hours. The reaction was diluted with EtOAc, washed with saturated sodium bicarbonate solution and brine and the organic layer concentrated in vacuo and the residue was purified by column chromatography on silica gel (0 to 100% EtOAc in hexanes) to provide 1-10. Data for 1-10: LC/MS: m/z (M+Na)=375.2 found; 375.4 calculated.

Provenance & Evidence