Morpholine → 3-Methyl-4-[((3s)-3-methyl-4-{[2-methyl-6-(4-morpholinyl)-3-pyridinyl]carbonyl}-1-piperazinyl)sulfonyl]benzonitrile hydrochloride

Participants

Reaction Conditions

Reaction Steps

4-({(3S)-4-[(6-Chloro-2-methyl-3-pyridinyl)carbonyl]-3-methyl-1-piperazinyl}sulfonyl)-3-methylbenzonitrile (may be prepared as described in Example 25) (55 mg, 0.13 mmol) was weighed into a microwave vial, and suspended in isopropanol (1.3 ml). Morpholine (0.221 ml, 2.54 mmol) was added and the mixture was heated in the microwave to 120° C. for 12 h with stirring. LCMS analysis indicated >65% conversion. The reaction mixture was concentrated to give the crude material as a pale yellow gum (78 mg). This was purified by MDAP to give the free base of the title compound as a colourless gum (31 mg).

Provenance & Evidence