Cesium carbonate → 2-Cyclopropyl-4-methoxy-5-nitropyridine

Participants

Reaction Steps

A mixture of 2-chloro-4-methoxy-5-nitropyridine (1.6 g, 8.48 mmol), cyclopropylboronic acid (1.458 g, 16.97 mmol), PdCl2(dppf)-CH2Cl2 adduct (1.386 g, 1.697 mmol), cesium carbonate (8.29 g, 25.5 mmol), and 1,4-Dioxane (15 mL) were heated using the microwave at 140° C. for 10 minutes. The reaction mixture was purified by normal phase chromatography (ISCO, 120 g silica, 0-3% methanol/DCM) to afford 2-cyclopropyl-4-methoxy-5-nitropyridine as a red solid (492 mg, 28%). MS (m/z) 195.0 (M+H+).

Provenance & Evidence