Abstract
We present an easy and straightforward synthesis of 3-arylpyrrolines 4a– g by repeated treatment of 4-aryl-1,2,5,6-tetrahydropyridines 2a– g with m-chloroperoxybenzoic acid (MCPBA) and boron trifluoride etherate (BF 3-OEt 2). The transformation proceeds via epoxidation, ring contraction, Baeyer–Villiger oxidation and elimination reaction and affords 3-arylpyrrolines 4a– g with 61–70% yield. This facile strategy was also used to synthesize racemic baclofen ( 6 ).
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