Tert-butyl 4-hydroxypiperidine-1-carboxylate → 4-[4-(5-Methanesulfonyl-2,3-dihydro-indol-1-yl)-[1,3,5]-triazin-2-yloxy]-piperidine-1-carboxylic acid tert-butyl ester

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Reaction Steps

11a was dissolved in THF. 4-Hydroxy-piperidine-1-carboxylic acid tert-butyl ester (40 mg, 1 eq) and potassium tert-butoxide (22 mg, 1 eq) were added and the mixture was stirred at room temperature for 3 h, then was quenched with water. The mixture was extracted with ethyl acetate twice, and the organic layer was washed with water and dried over sodium sulfate. The solvent was evaporated and the residue taken up in methanol and dichloromethane and purified by preparative HPLC to give 11-1, LCMS 476.2 (MH+), tR=3.68 (Method 6).

Provenance & Evidence