FeCl3-Catalyzed Cross-Coupling for Improving the Synthesis of Upadacitinib
Ziling Li,
Chundiao Shi,
Shengchang Xiang
et al.
Abstract:As an oral Janus kinase 1 inhibitor, upadacitinib shows good activity in the treatment of rheumatoid arthritis, especially for other drug-resistant and refractory rheumatoid arthritis patients. A key step in the synthesis of upadacitinib is the introduction of ethyl on the pyrroline ring. Here, a FeCl3/p-aminophenol catalyst system was used to increase the ethyl introduction for synthesis of pyrroline building blocks of upadaticinib. This catalytic system allows milder reaction conditions and increases the yie… Show more
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