Trifluoroacetic acid → (4S,7S,10aS)-4-Amino-7-(1,3,4-oxadiazol-2-yl)hexahydro-2H-pyrido[2,1-b][1,3]thiazepin-5(7H)-one 2,2,2-trifluoroacetate

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Reaction Steps

To a solution of tert-butyl (4S,7S,10aS)-7-(1,3,4-oxadiazol-2-yl)-5-oxooctahydro-2H-pyrido[2,1-b][1,3]thiazepin-4-ylcarbamate (22 mg, 0.060 mmol) in DCM (0.6 mL) at 0° C., was added TFA (0.323 mL, 4.20 mmol). The mixture was stirred at rt for 1.5 hr. The reaction was concentrated to give (4S,7S,10aS)-4-amino-7-(1,3,4-oxadiazol-2-yl)hexahydro-2H-pyrido[2,1-b][1,3]thiazepin-5 (7H)-one 2,2,2-trifluoroacetate (23 mg, 0.060 mmol, 100% yield). Anal. Calcd. for C11H16N4O2S m/z 268.4. found: 269.2 (M+H)+.

Provenance & Evidence