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Table 1 Optimization of reaction conditions

From: Development of a practical synthesis of etravirine via a microwave-promoted amination

Solvent Methoda Temperature (°C) Time Pressure (psi) Yield %
Dioxane A 120 12 h 83.5
CH3CN A 120 12 h 82.7
NMP A 120 12 h 83.6
Dioxane B 120 30 min 130 0
CH3CN B 120 30 min 130 0
THF B 120 30 min 130 0
DMF B 120 30 min 128 67.7
DMSO B 120 30 min 127 72.1
NMP B 120 30 min 127 81.4
  1. aMethod A: Conventional synthesis: 25% aq ammonia, autoclave, 120 °C, 12 h; Method B: Microwave-assisted synthesis: 25% aq ammonia, 10–30 min, 120–150 °C