Process to prepare treprostinil, the active ingredient in Remodulin®
AssigneeUnited Therapeutics Corporation
InventorsHitesh Batra, Sudersan M. Tuladhar, Raju Penmasta, David A. Walsh
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Abstract
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.
Claims11
A stable pharmaceutical batch of a salt of treprostinil that can be stored at ambient temperature and that is prepared by a method comprising providing a starting batch of treprostinil having one or more impurities resulting from prior alkylation and hydrolysis steps;
- forming a solution comprising treprostinil from said starting batch of treprostinil, and contacting the solution comprising treprostinil with a base to form a salt of treprostinil, wherein a level of one or more impurities found in the starting batch of treprostinil is lower in the pharmaceutical batch, said pharmaceutical batch being at least 2.9 grams.
A method of preparing a pharmaceutical batch of treprostinil or a salt thereof, comprising (a) alkylating a benzindene triol, (b) hydrolyzing the product of step (a) to form a solution comprising treprostinil, (c) contacting the solution comprising treprostinil from step (b) with a base to form a salt of treprostinil and (d) storing the salt of treprostinil at ambient temperature and thereafter acidifying the salt of treprostinil to form treprostinil, wherein forming the salt of step (c) reduces the amount of one or more impurities resulting from steps (a) and/or (b) in the pharmaceutical batch.
Dependencies are inferred from the claim text.