Chiral 2-trifluoromethylmorpholine is an useful intermediate employed in the syntheses of RSV, IRAK4 inhibitors, AMPA receptor antagonist, GPR43 agonist and mGluR2 negative allosteric modulator etc. We developed a route to yield optically pure 2-trifluoromethylmorpholine without SFC separation. Our method has a number of attractive features, including readily available and inexpensive starting material 2-(trifluoromethyl)oxirane, mild reaction conditions and easy purification [<b>Figure1</b>]. This new protocol was successfully used to generate 400 g of compound <b>1 </b>with an overall yield of 36%.

Novel synthesis of chiral 2-trifluoromethylmorpholine

2019 Fall National Meeting

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