4-Fluoro-3-nitrobenzotrifluoride → (S)-3-Amino-7-trifluormethyl-2,3-dihydrobenzo[b][1,4]oxazepin-4 (5H)-one trifluoro acetate

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Reaction Steps

In a similar manner to that described for the preparation of (S)-3-amino-8-methyl-2,3-dihydrobenzo[b][1,4]oxazepin-4(5H)-one trifluoroacetate except in Step 3 the reaction mixture was stirred for 4 h and in the material obtained in Step 4 was triturated with hexane, (S)-2-(tert-butoxycarbonylamino)-3-hydroxypropanoic acid (4.1 g, 20.0 mmol) and 1-fluoro-2-nitro-4-(trifluoromethyl)benzene (4.18 g, 20.0 mmol) were converted to the title compound (1.06 g) which was used without purification.

Provenance & Evidence