Progress in the Synthesis of Heterocyclic Compounds Catalyzed by Lipases

Abstract

Heterocyclic compounds are representative of a larger class of organic compounds, and worthy of attention for many reasons, chief of which is the participation of heterocyclic scaffolds in the skeleton structure of many drugs. Lipases are enzymes with catalytic versatility, and play a key role in catalyzing the reaction of carbon–carbon bond formation, allowing the production of different compounds. This article reviewed the lipase-catalyzed aldol reaction, Knoevenagel reaction, Michael reaction, Mannich reaction, etc., in the synthesis of several classes of heterocyclic compounds with important physiological and pharmacological activities, and also prospected the research focus in lipase-catalyzed chemistry transformations in the future.

Synthesis of Five-Membered Heterocycles Using Water as a Solvent

“…Candida rugosa lipase (CRL) mediated reaction of 1,3-diketone with fumaronitrile resulted in the formation of poly cyano substituted indoles in excellent yields (Figure 20) [28].…”

“…Polyhydroxyalkyl furans were also prepared from lipase-catalysed Knoevenagel reaction in water using malononitrile and reducing sugars as substrates. Out of the various lipases deployed in the reaction Novozyme-435 showed the highest catalytic activity (Figure 21) [28].…”