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With tetrakis(triphenylphosphine) palladium(0); sodium carbonate In 1,4-dioxane; water at 100℃; for 21h;
7-1.1 Step 7: tert-Butyl 4-(6-(2-bromo-5-methoxyphenyl)-5-chloro-7- fluorobenzo jcjisothiazol-3-yl)piperazine-1-carboxylate
General procedure: A mixture of tert-butyl 4-(6- bromo-5 -chloro-7-fluorobenzo [cjisothiazol-3-yl)piperazine- 1 -carboxylate (Intermediate D, 111 mg, 0.247 mmol), 2-bromo-5-methoxybenzene boronic acid (0.114 mL, 0.494 mmol), sodium carbonate (0.041 mL, 0.988 mmol), and tetrakis(triphenylphosphine)palladium (14.3 mg, 0.012 mmol) in 1,4-dioxane (1.6 mL) and water (0.4 mL) was heated at 90 °C for 21 h. The reaction mixture then concentrated in vacuo, adsorbed onto silica gel, and purified by column chromatography (silica gel, 0-20% (3:1) EtOAc/EtOH in heptane) to furnish tertbutyl 4-(6-(2-bromo-5 -methoxyphenyl)-5-chloro-7-fluorobenzo[cjisothiazol-3-yl)piperazine- 1-carboxylate: m/z (ESI, +ve) 558.1 (M+H)t
With tetrakis(triphenylphosphine) palladium(0); sodium carbonate In 1,4-dioxane; water at 100℃;
7.1 Step 1:
Step 1: 2-Amino-5-chloro-3-fluoro-4-(3-methoxynaphthalen-1-yl)benzoic acid Prepared from Intermediate A using a procedure analogous to that described in Method 1, Step 7: m/z (ESI, +ve) 346.0 (M+H)+.
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