Efficient Synthesis of Key Intermediate Toward Liphagal Synthesis

Abstract

Liphagal (A) is a very potent and selective inhibitor of PI3Kα (p110α) and is under development for an oncolytic drug. We herein report the new and concise synthesis of key intermediates (7, 8), which have been used for liphagal synthesis and will be useful for generating liphagal-based chemical entities for drug discovery purposes.

Keywords:

• Anticancer
• isoform selective inhibitor
• liphagal
• natural product synthesis
• PI3K

ACKNOWLEDGMENT

We thank the Department of Analytical Chemistry for their effort in providing ¹H NMR, ¹³C NMR, mass, HRMS, and HPLC data.