Abstract

Abstract The Bischler–Napieralski reaction is a significant strategy for the syntheses of isoquinolines. First, in 1893, this method was reported by August Bischler and Bernard Napieralski based on the cyclization of β-arylethylamides or β-arylethylcarbamates by intramolecular electrophilic aromatic substitution reaction, using a condensing agent such as phosphorus oxychloride (POCl3). In this chapter, we try to highlight the various aspects, issues, and applications of this reaction in the syntheses of isoquinoline derivatives. The isoquinoline nucleus is often found as a scaffold in the alkaloid families with interesting biological and physiological activities.

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