Hydrochloric Acid → (R)-5-[5-(6-chloro-benzooxazol-2-yl)-2-fluoro-phenyl]-6,6-difluoro-5,7,7-trimethyl-2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine hydrochloride

Participants

Reaction Steps

In a manner analogous to that described in Example 18b), the treatment of [bis-(4-methoxy-phenyl)-phenyl-methyl]-{(R)-5-[5-(6-chloro-benzo oxazol-2-yl)-2-fluoro-phenyl]-6,6-difluoro-5,7,7-trimethyl-2,5,6,7-tetrahydro-[1,4]oxazepin-3-yl}-amine (38 mg, 51.3 μmol) with trifluoro acetic acid (40 μl, 513 μmol), treatment with hydrochloric acid and followed by trituration with diethyl ether yielded the (R)-5-[5-(6-chloro-benzooxazol-2-yl)-2-fluoro-phenyl]-6,6-difluoro-5,7,7-trimethyl-2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine hydrochloride (16 mg, 66% yield) as an off-white solid. MS (ISP): m/z=438.2 [M+H]+ and 440.3 [M+2+H]+.

Provenance & Evidence