Synthesis of Simple 3,3-Diarylazetidines from -Boc-3-arylazetidinols Using Friedel-Crafts Arylation Conditions.

A synthesis of 3,3-diarylazetidines from -Boc-3-aryl-3-azetidinols using Friedel-Crafts arylation conditions with AlCl is described. A series of substituted diarylazetidines were readily prepared and isolated as the oxalate salts in high yield and high purity. The 3,3-diarylazetidine oxalates were then easily converted into -alkyl and -acyl analogues (RX, NaHCO/DMF/100 °C) in high overall yields.