Abstract

A variety of methods for regioselective formylation have been examined and exemplified with 3-methylthiophene. Optimal yields and regioselectivity for 2-formylation were obtained with N-formylpyrrolidine (11:1) although up to a 46:1 ratio could be obtained with MeOCHCl 2:TiCl 4, albeit in lower yield. Optimal 5-formylation (1:1.5) was obtained when using N-formylindoline:(COCl) 2.

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