反应详情

Methyl 3-[N-(4-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoate (3.77 g, 6.27 mmol) from Step D of Example 1, was dissolved in 75 mL of dry CH2Cl2 and the solution was charged with 6.27 g (47.0 mmol) of AlCl3 and the mixture was stirred at RT, under Ar, for 1.75 hours. The reaction was then quenched by the addition of 0.5N Na, K tartrate (150 mL) and the resulting mixture was extracted with EtOAc (3×). The organic extracts were washed with 0.5N Na, K tartrate (1×) and with brine (1×), and dried (MgSO4). Filtration and removal of solvents provided a brown oily residue which was chromatographed on silica gel using EtOAc-hexane (1:3) to give the title compound.

1. customThe reaction was then quenched by the addition of 0.5N Na, K tartrate (150 mL)
2. extractionthe resulting mixture was extracted with EtOAc (3×)
3. washThe organic extracts were washed with 0.5N Na, K tartrate (1×) and with brine (1×)
4. dry with materialdried (MgSO4)
5. filtrationFiltration and removal of solvents
6. customprovided a brown oily residue which
7. customwas chromatographed on silica gel