Efficient Synthesis of Key Intermediate Toward Liphagal Synthesis

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.