57830-14-5Relevant articles and documents
Synthesis of 5-phenoxyisobenzofuran-1(3H)-one as a key intermedate of the drug roxadustat
Li, Xi-An,Yue, Li-rong,Zhang, Zhi-gui,Xu, Jiao,Li, An-pai,Hu, Dong-yan,Han, Guang-tian,Ren, Hua-zhong,Nan, Ze-dong,Feng, Jia-fu
, (2020)
In this paper, a novel synthetic route to the key intermediate of the drug Roxadustat, 5-phenoxyisobenzofuran-1(3H)-one, was achieved in two steps in overall 78percent yield by using (3-phenoxyphenyl) methanol as the starting material. The synthetic route has the advantages of fewer steps, good regioselectivity, low catalyst consumption, high yield and lower raw material costs which are beneficial to realize industrial production.
Preparation method of isoquinoline derivative
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Paragraph 0052-0058, (2021/02/10)
Disclosed is a preparation method of an isoquinoline derivative. A preparation method of a compound represented by a general formula II, i.e., 4-hydroxy-1-methyl-7-phenoxy isoquinoline-3-formate, is provided, wherein substituent definitions are as defined in the specification. The preparation method comprises the following steps of: under an acidic condition, dissolving a compound shown as a structural formula III in dimethyl sulfoxide, catalyzing by a ferrous ion (Fe) catalyst, and oxidizing by H2O2 to obtain the 4-hydroxy-1-methyl- 7-phenoxy isoquinoline-3-formate shown as the structuralformula II. By using the method, the production efficiency can be greatly improved, the production cost is reduced, the product purity can be ensured, and the method is suitable for industrial mass production.
IMPROVED PROCESS FOR THE PREPARATION OF ROXADUSTAT
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Page/Page column 13; 19, (2021/10/30)
A synthetic route for the preparation of Roxadustat, or a pharmaceutically acceptable salt thereof. Each route involves several novel intermediates and avoids the use of column chromatography.