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Synthesis of 5-phenoxyisobenzofuran-1(3H)-one as a key intermedate of the drug roxadustat
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2020-07-05 , DOI: 10.1016/j.tetlet.2020.152181 Xi-An Li , Li-rong Yue , Zhi-gui Zhang , Jiao Xu , An-pai Li , Dong-yan Hu , Guang-tian Han , Hua-zhong Ren , Ze-dong Nan , Jia-fu Feng
中文翻译:
5-苯氧基异苯并呋喃-1(3H)-one合成为药物roxadustat的关键中间体
更新日期:2020-07-18
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2020-07-05 , DOI: 10.1016/j.tetlet.2020.152181 Xi-An Li , Li-rong Yue , Zhi-gui Zhang , Jiao Xu , An-pai Li , Dong-yan Hu , Guang-tian Han , Hua-zhong Ren , Ze-dong Nan , Jia-fu Feng
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 78% 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.
中文翻译:
5-苯氧基异苯并呋喃-1(3H)-one合成为药物roxadustat的关键中间体
本文以(3-苯氧基苯基)甲醇为原料,分两步实现了药物Roxadustat关键中间体5-苯氧基异苯并呋喃-1(3H)-的一种新颖合成途径,总收率78%。 。该合成路线具有步骤少,区域选择性好,催化剂消耗低,收率高,原料成本低的优点,有利于工业化生产。