An efficient method for construction of tetrahydroisoquinoline skeleton via double cyclization process using ortho-vinylbenzaldehydes and amino alcohols:: application to the synthesis of (S)-cryptostyline II

Thermal double cyclization reaction using ortho-vinylbenzaldehyde and 3-aminopropanols proceeded smoothly to give isoquinoline derivatives via 6 pi-azaelectrocyclization pathway. The method was applied to the efficient synthesis of (S)-cryptostyline II. (c) 2008 Elsevier Ltd. All rights reserved.