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2-哌啶酮经双氯取代和缩合-消除反应得3-吗啉-4-基-5,6-二氢-1H-吡啶-2-酮,与1-(4-碘苯基)-2-哌啶酮进行亲核取代反应得5,6-二氢-3-(4-吗啉基)-1-[4-(2-氧代-1-哌啶基)苯基]-2-吡啶酮,继而经1,3偶极环加成、氨解得抗凝血药阿哌沙班,总收率30.2%(以2-哌啶酮计),纯度99.8%。工艺稳定,反应条件温和,操作简便,适宜工业生产。
Reaction of 2-piperidone with dichloro-substituted and condensation-elimination reaction gave 3-morpholin-4-yl-5,6-dihydro-1H-pyridin-2-one and 1- (4-iodophenyl) (4-morpholinyl) -1- [4- (2-oxo-1-piperidinyl) phenyl] -2-piperidinone - pyridone, followed by 1,3 dipolar cycloaddition, ammonia solution of anticoagulant apixaban, the total yield of 30.2% (2 - piperidone dollars), purity of 99.8%. Stable process, mild reaction conditions, easy operation, suitable for industrial production.