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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