Barium hydroxide, octahydrate → Propane-2-sulfonic acid {2-[4'-(2h-tetrazol-5-ylmethyl)-biphenyl-4-yl]-thiophen-3-yl}-amide

Beteiligte Stoffe

Reaktionsschritte

Deoxygenate and heat a mixture of trifluoro-methanesulfonic acid 4′-(5H-tetrazol-5-ylmethyl)-biphenyl-4-yl ester (48mg, 0.2 mmol), propane-2-sulfonic acid {2-[4-(4,4,5,5-tetramethyl-[1,3,2] dioxaborolan-2-yl)-phenyl]-thiophen-3-yl}-amide (95 mg, 0.24 mmol, 1.2 eq.), barium hydroxide octahydrate(189 mg, 0.6 mmol, 3 eq.) and Pd(dffp)(29 mg, 0.04 mmol, 0.2 eq.) in 2 ml DMF and water mixture (4/1, v/v) to 80° C. overnight. Cool the mixture to room temperature and dilute with 30 mL EtOAc. Wash with water (3×10mL) and saturated aq. sodium chloride, dry, and remove solvent. Purification by flash chromatography (Silica gel-CH2Cl2:MeOH(1/50, v/v)) affords the title compound 50 mg(53%). MS (m/e): 441.1(M+1).

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