Abstract
AbstractThe dehydrative cyclization of N‐(o‐hydroxybenzoyl)threonine derivative 1a is efficiently promoted by the combined use of molybdenum(VI) oxides and benzoic acids bearing electron‐withdrawing substituents. In the presence of ammonium molybdate [(NH4)2MoO4, 10 mol %] and pentafluorobenzoic acid (C6F5CO2H; 10 mol %), dehydrative cyclization of 1a was conducted in toluene under azeotropic reflux conditions to give 2‐(o‐hydroxyphenyl)oxazoline 2a in 76 % yield. Furthermore, the first total synthesis of the antitumour substance BE‐70016 was achieved using the catalytic dehydrative cyclization of 1a as a key reaction.
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