A convergent synthesis of NNRTI 1 is described. The key step involves a direct coupling of acid chloride 4 with Grignard reagent 11 in the presence of bis[2-( N, N -dimethylamino)ethyl] ether that moderates the reactivity of the Grignard reagent to give benzophenone 7 . An efficient 2-step process for the preparation of 2-fluoro-3-methyl-4-aminobenzoic acid ( 3 ) is also described.
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Wang et al. (2012) studied this question.
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