Hydrochloric Acid → HCID 89699899, compound

Participants

Reaction Conditions

Reaction Steps

100 mg (0.38 mmol) of the compound of Example 24A and 104 mg (0.42 mmol) of tert-butyl 3-[(methylsulphonyl)oxy]azetidine-1-carboxylate together with 259 mg (0.80 mmol) of caesium carbonate were initially charged in 1 ml of DMF and stirred at 90° C. overnight. The mixture was then stirred into 10 ml of 0.1 M hydrochloric acid and extracted with ethyl acetate. The organic phase was washed with saturated sodium chloride solution, dried over sodium sulphate, filtered and concentrated under reduced pressure. The residue was purified by preparative HPLC (Method 18). This gave 60 mg (88% pure, 33% of theory) of the title compound.

Provenance & Evidence