2-Chloro-4-(thiophen-2-yl)pyrimidine → [1-(3-Ethoxy-4-methoxy-benzyl)-piperidin-4-yl]-(4-thiophen-2-yl-pyrimidin-2-yl)-amine

Participants

Reaction Steps

A solution of 2-chloro-4-thiophen-2-yl-pyrimidine (29.5 mg, 0.15 mmol, 1.0 equiv) and 1-(3-ethoxy-4-methoxy-benzyl)-piperidin-4-ylamine (47.6 mg, 0.18 mmol, 1.2 equiv; intermediate A1) in DMAc (2 mL) was heated by microwave irradiation to 220° C. for 30 min. Removal of the solvent under reduced pressure and purification by preparative HPLC on reversed phase eluting with a gradient of acetonitrile/water provided 11.5 mg (15%) of the title compound. MS (ISP): 425.3 [M+H]+.

Provenance & Evidence