Diethyl Ether → (7R)-7-Amino-4-chloro-9-(2,2,2-trifluoroethyl)-6,7,9,10-tetrahydroazepino[3,4-e]indazol-8(3H)-one bis-methanesulfonate

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To a mixture of benzyl[(7R)-4-chloro-8-oxo-9-(2,2,2-trifluoroethyl)-3,6,7,8,9,10-hexahydroazepino[3,4-e]indazol-7-yl]carbamate from Step A (265 mg, 0.568 mmol) and anisole (184 mg, 1.70 mmol) in CH2Cl2 (4 mL) was added methanesulfonic acid (1.84 mL, 28 mmol). The resulting mixture was stirred at ambient temperature for 45 min, Et2O (45 mL) was added, and stirring was continued for 20 min. The supernatant was removed and the residue was washed with Et2O and dried in vacuo to give the title compound. MS: m/z=333.

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