Synthesis of 4‐(4′‐Arylpiperazinyl)phenylalanine Derivatives and Drug Conjugates via Buchwald–Hartwig Amination

Key Points

• The research aims to develop a method for synthesizing N-arylpiperazine phenylalanine derivatives for potential drug applications.
• Developed a palladium-catalyzed approach for synthesis.
• Focused on N-arylation of phenylalanine peptides.
• Demonstrated adaptability to various protecting groups.
• Achieved gram-scale synthesis of derivatives.
• Applied methodology to create drug conjugates with naproxen and ciprofloxacin.
• Achieved synthesis yields up to 85%.
• Successfully synthesized a variety of N-arylpiperazine-substituted derivatives.
• Demonstrated efficiency in creating peptidomimetics.
• Successfully conjugated phenylalanine with nonsteroidal anti-inflammatory drug naproxen.
• Introduced a new method applicable to antibiotics such as ciprofloxacin.