Synthesis of Substituted α-Trifluoromethyl Piperidinic Derivatives

Abstract

A comprehensive survey of pathways leading to the generation of α-trifluoromethyl monocyclic piperidinic derivatives is provided (65 references). These compounds have been synthesized either from 6-membered rings e.g., pipecolic acid or lactam derivatives by introduction a trifluoromethyl group, from pyridine or pyridinone derivatives by reduction, and from 5-membered rings e.g., prolinol derivatives by ring expansion, from linear amines by cyclization or from dienes/dienophiles by [4 + 2]-cycloaddition.

Keywords

• nitrogen heterocycles
• fluorine
• piperidine
• trifluoromethyl group
• ring expansion
• cyclization
• cycloaddition