Methyl iodide → Riociguat

Participants

Reaction Steps

Prepared in analogy to Example 6 with 310 mg (0.76 mmol) of methyl-4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinylcarbamate from Example 5, 27.32 mg (1.14 mmol) of sodium hydride and 215.5 mg (1.52 mmol) of iodomethane. The mixture is worked up by adding water and 2 molar potassium hydroxide solution and extracting with dichloromethane. The combined organic phases are dried with magnesium sulphate and concentrated in a rotary evaporator. The residue is purified by preparative RP-HPLC.

Provenance & Evidence