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Synthetic method JAKAK1 inhibitor Filgogogotinib (by machine translation)
The invention provides Filgogogotinib, which comprises the following steps: (1) reacting 2 – amino -6 -bromopyridine with p-methylbenzene derivatives, and preparing compound 1; (2) reacting compound 1 with hydroxylamine hydrochloride, N, N – diisopropylethylamine to obtain compound 2; (3) reacting compound 2 with thiomorpholine 3, 4 dioxides, thereby obtaining Filgogogotinib.) . compound (3) and compound (4) are reacted, yielding compound 5, compound [4], and azodiisobutyronitrile to react, and the compound 5; (6 1 -) 5 is reacted with the azodiisobutyronitrile -1. The route of synthesizing Filgogogou is firstly coupled and then closed loop, the raw material is cheap, the reaction operation is simple, the product is easy to purify, the yield is high, and the method is suitable for commercial scale production. (by machine translation)
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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem