4-Toluenesulfonyl chloride → HCID 89423033, compound

Participants

Reaction Steps

To a stirred solution of methyl 6-(2-((tert-butyldimethylsilyloxy)methyl)-1-methyl-1H-indol-5-yl)-1-(2,4-dimethoxybenzyl)-5-ethyl-4-hydroxy-2-oxo-1,2-dihydropyridine-3-carboxylate (2.0 g, 3.2 mmol), prepared according to procedure described in Example 164, Step 2, in CH2Cl2 (15 mL) was added Et3N (0.68 mL, 4.9 mmol, 1.5 eq) and TsCl (0.74 g, 3.9 mmol, 1.2 eq) at 0° C. The mixture was allowed to warm to room temperature then stirred for 2 h. The solvent was removed and the residue was purified by flash column chromatography (0-25% EtOAc in CH2Cl2) to give the title compound (2.12 g, 85%). LC-MS 775.3 [M+H]+, RT 1.80 min.

Provenance & Evidence