Morpholine → 4-{6-Methyl-5-[((2s)-2-methyl-4-{[4-(trifluoromethyl)phenyl]sulfonyl}-1-piperazinyl)carbonyl]-2-pyridinyl}morpholine hydrochloride

Participants

Reaction Conditions

Reaction Steps

(2S)-1-[(6-Chloro-2-methyl-3-pyridinyl)carbonyl]-2-methyl-4-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine (may be prepared as described in Example 24) (67 mg, 0.15 mmol) was weighed into a microwave vial, and dissolved in isopropanol (1.4 ml). Morpholine (0.253 ml, 2.90 mmol) was added and the clear solution was heated in the microwave to 120° C. for 4 h with stirring. LCMS analysis showed ˜40% conversion. Further morpholine (0.126 ml, 1.45 mmol) was added and the stirred reaction was heated to 120° C. for 6 h. LCMS analysis showed ˜79% conversion. The reaction mixture was concentrated to give the crude material as a colourless gum (87 mg). This was purified by MDAP to give the free base of the title compound as a colourless gum (44 mg).

Provenance & Evidence