872365-14-5Relevant articles and documents
Using a Johnson-Claisen Rearrangement Strategy to Construct Azaindoles – A Streamlined and Concise Route for the Commercial Process of Fevipiprant
Dedic, Darija,Dempsey, Glen,Fei, Zhongbo,Hueber, Lukas,K?nigsberger, Kurt,Lustenberger, Philipp,Mathes, Christian,Napp, Matthias,Rüegger, Ueli,Riss, Bernard,Schlama, Thierry,den Reijer, Carolien
, p. 4490 - 4494 (2021)
A novel and concise synthesis of the DP2 receptor antagonist Fevipiprant (NVP-QAW039) was developed. The initial research route was suffering from a long reaction sequence to the functionalized 7-aza-indole core followed by a poorly selective N(1)-alkylat
PREPARATION OF 2-[2-METHYL-1-[[4-METHYLSULFONYL-2-(TRIFLUORO METHYL)PHENYL]METHYL] PYRROLO[2,3-B]PYRIDIN-3-YL]ACETIC ACID
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, (2019/07/17)
The present invention relates to a novel compound of Formula IV and use of said compound for the preparation of 2-[2-methyl-1-[[4-methylsulfonyl-2-(trifluoromethyl)phenyl] methyl]pyrrolo[2,3-b]pyridine-3-yl]acetic acid [fevipiprant], Formula IV wherein A is SO2Me, halogen or a leaving group. The present invention further relates to a process of preparation of pharmaceutical acceptable salts of fevipiprant and composition thereof.
Concise synthetic method of asthma drug Fevipiprant
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, (2018/09/21)
The invention discloses a concise synthetic method of asthma drug Fevipiprant. The concise synthetic method of asthma drug Fevipiprant comprises a following step: a compound 4 is reacted so as to obtain Fevipiprant. According to the concise synthetic method, 1-(3-pyridyl)-2-acetone is taken as a raw material, a pyridine nitrogen oxide is generated through oxidation, a 7-azaindole mother nucleus isobtained under mild conditions. The step number of the concise synthetic method are few, the technology is simple, reaction conditions are mild, production cost is low, no transition metal catalysisis needed, no protective group is needed in the whole synthesis process, and a relatively simple four step Fevipiprant preparation method is invented.