Process for Preparation of Phthalazinone (Olaparib) Derivatives and uses thereof

• Higher purity: Results in lower purification costs
• Improved green chemistry metrics: Better atom economy, carbon efficiency, reaction mass efficiency, and mass productivity, with lower energy use
• Synthesized using DMF and ethanol, minimizing impurities from earlier Wittig reactions

• Eco-friendly synthesis of Olaparib using inexpensive, commercially available starting materials (piperazine and cyclopropane carbonyl chloride) in four steps, with 51% overall yield.
• Key steps include generating a conjugated enolate from 2-acetylbenzoic acid, followed by α-arylation under transition metal-free conditions and ring construction to form the final Phthalazinone scaffold, yielding Olaparib.
• The synthetic strategy includes optimized reaction protocols for nearly every step.

• Higher yield: 51% vs. 30–46% (previous methods)
• Fewer steps: 4 vs. 7 steps
• Estimated raw material cost: Comparable to landed cost (~USD 3090/kg)