Furan, pyrrole and thiophene derivatives are aromatic five-membered
heterocyclic compounds with one heteroatom. These compounds are widely distributed
in a wide range of natural and non-natural compounds. Many of these derivatives have a
diverse range of bioactivities such as antimicrobial, anticancer, antiparasitic, antiinfammatory,
antihypertensive antiviral, antitumor, activities, and several derivatives
have been marketed as drugs for treatment of various diseases. Besides, the use of
furan, pyrrole and thiophene derivatives also has been found in other fields such as
organic materials, agrochemicals, flavors, dyes. They can serve as intermediate or
building blocks for the preparation of natural product compounds or drugs.
With such a diverse range of applications, the preparation of furan, pyrrole and
thiophene derivatives has drawn intensive attention of chemists. Several established
synthetic approaches for example the Paal-Knorr, Feist–Benary, Gewald, Knorr and
Fiesselmann, Huisgen, and Hantzsch syntheses have been modified and improved.
Moreover, an enormous number of new methods for the preparation of these
heterocycles have been developed. This chapter will give an overview of published
studies on the construction of pyrrole, furan, and thiophene skeletons which date back
to 2012.
Keywords: 1, 4-diketones, 2-aminothiophenes, 2, 5-dimethoxytetrahydrofuran, 3-
yne-1, 2-diols, Anticancer, Antihypertensive, Antiinfammatory, Antimicrobial,
Antiparasitic, Antitumor, Antiviral, Clauson-Kaas synthesis, Cyclization, Feist–
Benary Synthesis, Fiesselmann synthesis, Gewald reaction, Hantzsch synthesis,
Paal-Knorr synthesis, Primary amines, Tosylmethyl isocyanide, Van Leusen
synthesis.
