Preparation of 3‐aminoalkylbenzo[b]thiophenes

Abstract We report an efficient entry into substituted 3‐(ω‐aminoalkyl)‐benzo[ b ]thiophenes that allows rapid generation of structural diversity. Alkylation of α,ω‐dihaloketones with thiophenols followed by acid‐catalysed cyclisation led to an efficient synthesis of 3‐(ω‐aminoalkyl)benzo[ b ]thiophenes. 2‐Carboethoxy derivatives were prepared using a directed ortho ‐metallation approach. These derivatives were readily converted into the corresponding amines.