Methanesulfonyl chloride → HCID 86695585, compound

Participants

Reaction Steps

(1S,5R)-8-Tert-butyl 2-methyl 3-hydroxy-8-azabicyclo[3.2.1]octane-2,8-dicarboxylate (1.75 g, 6.14 mmol) was dissolved in dichloromethane (30 mL), methanesulfonyl chloride (0.95 mL, 123 mmol) was added, followed by dropwise addition of N,N-diisopropylethyl-amine (5.29 mL, 30.7 mmol). The reaction mixture was stirred at room temperature overnight. After quench with saturated NaHCO3, the reaction mixture was extracted with dichloro-methane. The combined organic layer was washed with water and brine. Dried and concentrated to give 2.23 g of crude product. The crude was carried over the next step without further purification.

Provenance & Evidence