1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → (S)-3-Amino-8-trifluormethyl-2,3-dihydrobenzo[b][1,4]oxazepin-4 (5H)-one trifluoroacetate

Participants

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 1.2 eq. EDCI was used and the reaction mixture was stirred for 2 h and in Step 4 the mixture was stirred for 1 h and the material obtained was tritrurated with Et2O/pentane, (S)-2-(tert-butoxycarbonylamino)-3-hydroxypropanoic acid (4.96 g, 24.2 mmol) and 2-fluoro-1-nitro-4-(trifluoromethyl)benzene (5.05 g, 24.2 mmol) were converted to the title compound (1.6 g) as a pale yellow solid.

Provenance & Evidence