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US 8,940,930 B2Granted
Treprostinil production
AssigneeUnited Therapeutics Corporation
InventorsHitesh Batra, Raju Penmasta, Vijay Sharma, Sudersan M. Tuladhar, David A. Walsh
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Abstract
The present invention is directed to a novel method for preparing a synthetic intermediates for treprostinil. Also described are methods of preparing treprostinil comprising utilizing novel intermediates described herein as well as novel intermediates useful for synthesis prostacyclin derivatives, such as treprostinil.
Claims9
A method of preparing treprostinil or a pharmaceutically acceptable salt thereof comprising a cyclization reaction in which a compound of the formula:
- is converted into a compound of the formula:
- followed by hydrogenation, reaction with a reducing agent, deprotection, and conversion of a triol of formula (VIIa):
- into treprostinil or a pharmaceutically acceptable salt thereof,
- wherein, in each of the above formulas, P1 and P2 are each an independently selected alcohol protecting group;
- R is —(CH2)nX;
- n is 0, 1, 2, or 3;
- and
- X is phenyl substituted with one or more substituents independently selected from the group consisting of —NO2, —CN, halogen, (C1-C3)alkyl, halo(C1-C3)alkyl, (C1-C3)alkoxy and halo(C1-C3)alkoxy.
5 more elements
Dependencies are inferred from the claim text.