Diisopropylethylamine → [2-Amino-6-(1-methanesulfonyl-piperidin4-ylamino)-pyridin-3-yl]-(2-methoxy-phenyl)-methanone

Participants

Reaction Conditions

Reaction Steps

A mixture of (2-Amino-6-chloro-pyridin-3-yl)-(2-methoxy-phenyl)-methanone (24.9 mg, 0.0948 mmol, Example 5), 1-methanesulfonyl-piperidin-4-ylamine (50.6 mg, 0.284 mmol, from Step A above), N,N-diisopropylethylamine (38mg, 0.294 mmol) and ethanol (2.7 mL) were heated at 160-180° C. in a sealed tube under microwave conditions for 0.5-4 hrs. The resulting reaction mixture was concentrated in vacuo and the residue was purified on silica gel with methylene chloride/methanol to give [2-Amino-6-(1-methanesulfonyl-piperidin4-ylamino)-pyridin-3-yl]-(2-methoxy-phenyl)-methanone as a white solid (22.5 mg, 58% yield). HRMS, observed: 405.1594, calcd for (M+H)+: 405.1591.

Provenance & Evidence