Water → Methyl N-[6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}sulfanyl)-3,5-dicyano-4-piperidin-1-ylpyridin-2-yl]-N-methylglycinate

Participants

Reaction Steps

100 mg (0.21 mmol) of the compound from Example 46A were dissolved in 2 ml of dry THF. 57 mg (0.41 mmol) of methyl sarcosinate hydrochloride and 86 μl (0.62 mmol) of triethylamine were then added in succession. The reaction mixture was stirred at RT for 10 h. 1 ml of water was added, and the mixture was extracted three times with in each case 5 ml of ethyl acetate. The combined organic phases were washed once with 3 ml of saturated aqueous sodium chloride solution and dried over magnesium sulfate. After removal of the solvent on a rotary evaporator, the residue was purified by preparative HPLC (column: YMC GEL ODS-AQ S-5/15 μm; mobile phase gradient: acetonitrile/water 10:90→95:5).

Provenance & Evidence