Emcure Pharmaceutical Limited

Emcure Pharmaceuticals Limited

Chinmoy Mriganka Pramanik

Mukund Keshav Gurjar

Samit Satish Mehta

Narendra Kumar Tripathy

Jayendra Dattatraya Patole

Ganesh Kaluram Karhade

Balaji Vasant Chaugule

Kaliyaperumal Neelakandan

Ajit Sahebrao Borhade

The invention relates to improved method of synthesis for Treprostinil comprising condensation reaction of the carbonyl compound having allyl, alkyl, crotyl or MEM-protected phenolic hydroxyl group, compound (4) with a hydroxyl-protected alkynol (5) to give the condensation product, compound (6). Subjecting compound (6) to oxidation, reduction, hydroxyl protection and carbonylation, cyclization reactions gave the tricyclic derivative (10). Further reactions comprising reduction, hydrogenation and deprotection of the phenolic and side-chain hydroxyl groups, wherein the sequence and choice of reagents was governed by protecting groups, gave the triol intermediate, compound (14). Cyanoalkylation at phenolic hydroxyl functionality and further hydrolysis yielded the prostacyclin compound, Treprostinil (1) and its pharmaceutically acceptable salts, having desired purity.

Process for preparation of prostacyclin derivatives

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Pune, India

Chinmoy Mriganka Pramanik