2-(bromomethyl)oxetane

Conditions: temp:100.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: 500 mg (0.980 mmol) of the compound from example 82A were dissolved in 10 ml of DMF, 414 mg (1.270 mmol) of cesium carbonate and 150 mg (1.08 mmol) of 2-(bromomethyl)oxetane were added and the mixture was stirred at RT for 18 h, at 40° C. for 18 h and at 100° C. for 4 h. After cooling, water was added and the mixture was extracted with ethyl acetate. The combined organic phases were dried over sodium sulfate and concentrated on a rotary evaporator. The residue was dried under high vacuum. 581 mg (53% of theory, purity 63%) of the title compound were obtained. After cooling the mixture was extracted with ethyl acetate The combined organic phases were dried over sodium sulfate concentrated on a rotary evaporator The residue was dried under high vacuum

Conditions: temp:100.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: 500 mg (0.980 mmol) of the compound from example 82A were dissolved in 10 ml of DMF, 414 mg (1.270 mmol) of cesium carbonate and 150 mg (1.08 mmol) of 2-(bromomethyl)oxetane were added and the mixture was stirred at RT for 18 h, at 40° C. for 18 h and at 100° C. for 4 h. After cooling, water was added and the mixture was extracted with ethyl acetate. The combined organic phases were dried over sodium sulfate and concentrated on a rotary evaporator. The residue was dried under high vacuum. 581 mg (53% of theory, purity 63%) of the title compound were obtained. After cooling the mixture was extracted with ethyl acetate The combined organic phases were dried over sodium sulfate concentrated on a rotary evaporator The residue was dried under high vacuum