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In 1,4-dioxane; water at 105℃; for 3h; Sealed tube;
52 (S)-Isopropyl 2-(tert-butoxy)-2-(5-(4-((3, 4-dihydroisoquinolin-2(JH)-yl)methyl)phenyl)-4-(4, 4-dimethylpiperidin-1-yl)-2, 6-dimethylpyridin-3-yl)acetate:
Pd(PPh3)4 (8.37 mg) andCs2CO3 (0.047 g) were added to a solution of (S)-isopropyl 2-(5-bromo-4-(4,4-dimethylpiperidin- l-yl)-2, 6-dimethylpyridin-3 -yl)-2-(tert-butoxy)acetate (0.034 g) and(4-(4,4, 5,5-tetramethyl- 1,3 ,2-dioxaborolan-2-yl)benzyl)- 1,2,3 ,4-tetrahydroisoquinoline(0.030 g) in dioxane (1. mL) and water (0.3 mL), sealed and heated at 105 °C for 3 h. After cooling, the solvents were removed under vacuum to give a residue which was purified by the preparative HPLC to give (S)-isopropyl 2-(tert-butoxy)-2-(5-(4-((3,4- dihydroi soquinolin-2( 1 H)-yl)methyl)phenyl)-4-(4,4-dimethylpiperidin- 1 -yl)-2,6-dimethylpyridin-3-yl)acetate. LCMS (M+H): 612.5.
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