(3R,4R)-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine is used to make Alvimopan CAS number is 119193-19-0, molecular formula: C13H19NO, molecular weight: 205.3. In the reaction step of Alvimopan,( 57280523,3R,4R)-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine was added to N-1 step of Alvimopan in the reaction to get the crude Alvimopan.The specific operation process is as follows:
(3R,4R)-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine 30g,( 57280524,S)-2-methanesulfonylmethylphenylpropionyl-glycine isobutyl ester 55g, 150 ml of Diethylamine and 1500 ml of toluene were added to a three-necked flask, and the mixture was heated under reflux for 6 hours. After the reaction was completed, the mixture was cooled to room temperature, and then added with water (600 ml), and the organic layer was separated, dried over anhydrous sodium sulfate, filtered, and evaporated. Oily Ivoric isobutyl ester 34g. Add 34 g of Ivoric isobutyl ester to a 2000 ml three-necked flask, add 850 ml of ethanol and…