81846-19-7Relevant articles and documents
EFFICIENT CRYSTALLIZATION PROCESS FOR PREPARING ULTRAPURE TREPROSTINIL AND CRYSTAL PREPARED THEREFROM
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Paragraph 0083-0084, (2021/06/26)
There is provided a crystalline Form I of anhydrous Treprostinil and processes for the preparation thereof. The crystalline Form I of anhydrous Treprostnil is a stable crystalline form, which can provide steady physicochemical properties for pharmaceutical formulations, and is advantageous widely and safety used in storage, shipment, and handling for commercially considerations.
Synthetic routes to treprostinil N-acyl methylsulfonamide
Brocchini, Steve,Clapp, Lucie H.,Laing, Peter,Picken, Christina,Shen, Lei
, (2019/12/25)
The synthesis of the prodrug candidate, treprostinil N-acyl methylsulfonamide 5 was accomplished from treprostinil 2 utilising protecting group strategies. A more direct synthesis for the prodrug was also achieved using a treprostinil triol precursor 12 and bromoacetyl acylmethylsulfonamide 14. The overall yield of treprostinil N-acyl sulfonamide 5 directly from the triol precursor 12 is similar to the protecting group strategies because deprotonation of the acidic proton in the bromoacetyl acylmethylsulfonamide 14 reduces electrophilicity. However, the more direct route using the treprostinil triol precursor holds greater promise as a strategy to prepare a wide range of treprostinil prodrug candidates. Treprostinil N-acyl methylsulfonamide prodrug 5 exhibited a 30-fold decrease in the potency at the human prostacyclin (IP) receptor compared to treprostinil 2 in an in vitro cyclic AMP assay.
Intermediate for preparing treprostinil, preparation method of intermediate and method for preparing treprostinil through intermediate
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Paragraph 0108; 0119; 0120; 0121, (2017/08/29)
The invention relates to an intermediate for preparing treprostinil, a preparation method of the intermediate and a method for preparing the treprostinil through the intermediate. Specifically, the invention relates to a compound which is shown as a formula (VI) and is used for preparing the treprostinil (shown as a formula (I)), a preparation method of the compound and a method for preparing the treprostinil through the compound. The method for preparing the treprostinil comprises the following steps: carrying out reduction and hydroxyl removal protection on the compound shown as the formula (VI) to obtain a compound shown as a formula (III); taking the compound shown as the formula (III) and chloroacetonitrile to react and hydrolyzing to prepare the treprostinil shown as the formula (I). The method is simple and convenient to operate, high in synthesis yield and suitable for large-scale production. (The formula (I) is shown in the description, the formula (III) is shown in the description and the formula (VI) is shown in the description.).