United Therapeutics Corporation

Lung Biotechnology Pbc

Lung Biotechnology Inc.

Sudersan M Tuladhar

Hitesh Batra

David A Walsh

Raju A Penmasta

Vijay Sharma

Sri Harsha Tummala

Raju Penmasta

This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.

Process to prepare treprostinil, the active ingredient in Remodulin&#xae;

The present disclosure provides regioselective methods for synthesizing intermediates useful in making prostacyclin. The methods include heating the compound of Formula 2 at a temperature of 180&#xb0; C. to 185&#xb0; C. Wherein the heating comprises irradiating the compound of formula 2 with microwave radiation.

Synthesis of intermediates for producing prostacyclin derivatives

The present disclosure provides regioselective methods for synthesizing intermediates useful in making prostacyclin derivatives, such as treprostinil.

An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

Method of producing beraprost

The present invention is directed to methods for preparing Beraprost and novel synthetic intermediates for Beraprost.

Methods for producing Beraprost and its derivatives

Process to prepare treprostinil, the active ingredient in remodulin&#xae;

An improved method is described for making single isomers of synthetic benzoprostacyclin analog compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

The present invention is directed to methods for preparing Beraprost and novel synthetic intermediates for Beraprost. In one aspect, a process is provided to produce a pharmaceutical compound represented by the general Formula (I) via a radical cyclization route. The process is completed in fewer steps than the known synthetic methods and may be conducted to prepare commercially useful quantities. In another aspect, synthetic methods are provided for producing Beraprost and its derivatives, which are stereoselective, efficient, scalable and economical. In another aspect, substantially isomerically pure compounds and intermediates are produced by the above processes.

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Silver Spring, MD, United States of America

Sudersan M Tuladhar