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ChemicalBook CAS DataBase List 2-Morpholinopyridin-4-ylboronic acid

2-Morpholinopyridin-4-ylboronic acid synthesis

2synthesis methods
-

Yield:952206-85-8 90%

Reaction Conditions:

with (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride;potassium acetate in 1,4-dioxane;water at 80; for 12 h;Inert atmosphere;

Steps:

39.2 Step 2: (2-Morpholinopyridin-4-yl,)boronic acid

A mixture of 4-(4-bromopyridin-2-yl)morpholine (1.08 g, 4.44 mmol),bis(pinacolato)diboron (1.35 g, 5.33 mmol), AcOK (1.09 g, 11.11 mmol), [1,1-bis(diphenylphosphino)ferrocenej dichloropalladium(II) (325.07 mg, 444.26 umol) in 1,4- dioxane (15 mL) was degassed and purged with N2 (3x) at 20 °C, and then the mixture was stirred at 80 °C for 12 hrs under N2 atmosphere. The reaction mixture was filtered and the filtrate was evaporated to afford the title compound (2.1 g, 90%) as a black oil. MS-ESI (m/z)calc’d for C9H14BN203 [M+Hf: 209.1. Found 209.0.

References:

WO2021/178780,2021,A1 Location in patent:Page/Page column 169-170