2-methylmorpholin-3-one

Conditions: temp:0.00; pressure:0.00; stir:

Conditions: temp:0.00; pressure:0.00; stir:

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

Procedure: A solution of 66 mg (0.57 mmol) of 2-methylmorpholin-3-one [CAS Reg. No. 100636-23-5] is initially charged in 4.5 ml of dry DMF, and 23.6 mg (0.196 mmol) of sodium hydride (60% in paraffin oil) are added. The mixture is stirred at room temperature for 45 min. The reaction solution is then cooled to 0° C. and a solution of 90 mg (0.163 mmol) of methyl 4-{(4E)-5-{2-[(5-chloropentyl)oxy]phenyl}-3-[4-(methoxycarbonyl)benzyl]pent-4-en-1-yl}benzoate (racemate; Example 32A) in 1.5 ml of dry DMF is added. The mixture is stirred at room temperature for 1.5 h. The reaction solution is then carefully poured into 15 ml of ice-cold 10% strength ammonium chloride solution. The mixture is extracted twice with dichloromethane. The combined organic phases are dried over sodium sulfate, filtered and concentrated. This gives 103 mg (0.57 mmol, 100% of theory) of a colorless oil which is reacted without further purification. The reaction solution is then cooled to 0° C. The mixture is stirred at room temperature for 1.5 h The mixture is extracted twice with dichloromethane The combined organic phases are dried over sodium sulfate filtered concentrated This gives 103 mg (0.57 mmol, 100% of theory) of a colorless oil which is reacted without further purification