This micro review focuses on the application of the modified Pictet-Spengler reaction to the synthesis of diverse polyheterocycles
with structural resemblance to natural products. The modified Pictet-Spengler reaction takes use of tethered biheterocycles comprising
nucleophilic partner and a source for electrophilic partner followed by their condensation with aldehydes/ketones to furnish annulated
polyheterocycles. Using this strategy engineering of numerous tethered biheterocycles into annulated polyheterocycles has been successfully
carried out using both 6-endo as well as 7-endo cyclizations.
Keywords: Pictet-Spengler reaction, 6-endo cyclization, 7-endo cyclization, Polyheterocycles
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