Strains. -Starting from a common building block, chloropyrimidine (I), two pathways lead to title analogues (VII) and (XI): the Wittig-Wadsworth-Emmons reaction via the Wittig precursor (V), and the Heck reaction via Heck precursor (IX). The necessity to maintain the 2,6-disubstitution pattern on the left phenyl ring to achieve a high level of inhibition on NNRTI-resistant viruses is demonstrated. Moreover, the methyl groups in TMC278 are replaced by other functionalities, cf. (VII) and (XI), without loss of …
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