Rozema, Michael J. published the artcileDevelopment of a Scalable Enantioselective Synthesis of JAK Inhibitor Upadacitinib, Safety of trimethyloxosulphonium chloride, the publication is Organic Process Research & Development (2022), 26(3), 949-962, database is CAplus.
Process development of a six-stage synthesis of upadacitinib, a JAK1 inhibitor, was described. It was highlighted by an enantioselective and diastereoselective hydrogenation of a tetrasubstituted olefin to set the two pyrrolidine stereocenters. Preparation of the main fragments and strategies to link them together, optimization of the imidazole cyclization and in-depth understanding of the formation of the urea moiety at the final stage were discussed.
Organic Process Research & Development published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C3H9ClOS, Safety of trimethyloxosulphonium chloride.
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