Triethylamine → 2-{6-[(Tert-butoxycarbonyl)amino]-3-azabicyclo[3.1.0]hex-3-yl)ethyl methanesulfonate

Participants

Reaction Steps

To a mixture of tert-butyl [3-(2-hydroxyethyl)-3-azabicyclo[3.1.0]hex-6-yl]carbamate (Intermediate 96) (376 mg, 1.55 mmol) and triethyl amine (0.283 mL, 3 mmol) in anhydrous chloroform (15 mL) was added at 0° C. methanesulfonyl chloride (228 mg, 3 mmol) via syringe. The reaction was allowed to warm to room temperature over 1 hr and worked up as described for Intermediate 6. The crude mesylate was used for the next step without delay.

Provenance & Evidence