N-[5-[4-[(1,1-dioxo-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-A]pyridine -2-yl]cyclopropanecarboxamide_Kain Industrial Additive

Background and overview[1] N-[5-[4-[(1,1-dioxo-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5- A]pyridin-2-yl]cyclopropanecarboxamide can be used as a pharmaceutical synthesis intermediate. Preparation[1] N-[5-[4-[(1,1-dioxo-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5- Preparation of A]pyridin-2-yl]cyclopropanecarboxamide (8A): 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborane- 2-yl)-benzyl)thiomorpholine 1,1-dioxide (Intermediate 1A) (20.18g, 53mmol), N-(5-bromo-[1,2,4]triazolo[1 ,5-a]pyridin-2-yl)cyclopropanecarboxamide (Intermediate 7A) (16.45g, 59mmol), Pd(dppf)Cl2 (3.91g, 5mmol), K2CO3 (22.06g, 160mmol) were added to 250mL in sequence into a three-necked flask, then add 1,4-dioxane (100 mL) and water (25 mL), and raise the temperature to 90°C under argon protection…

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