2-氟-5-[(4-氧代-3,4-二氢二氮杂萘-1-基)甲基]苯甲酸是合成奥拉帕尼的关键中间体。以邻羧基苯甲醛为原料,与亚磷酸二甲酯反应得到磷叶立德,再与2-氟-5-甲酰基苯甲酸进行WittigHorner反应、环合反应得到目标化合物,并对各步反应条件进...2-氟-5-[(4-氧代-3,4-二氢二氮杂萘-1-基)甲基]苯甲酸是合成奥拉帕尼的关键中间体。以邻羧基苯甲醛为原料,与亚磷酸二甲酯反应得到磷叶立德,再与2-氟-5-甲酰基苯甲酸进行WittigHorner反应、环合反应得到目标化合物,并对各步反应条件进行了优化,三步反应总收率70.9%。目标化合物经(1 H NMR)和(MS)确证结构。展开更多
A compound ethyl(5S,6R)-2-(4-methylphenyl)-6-[(1R)-tert-butyldimethylsilyloxyethy]-penem-3-carboxylate was synthesized through displacement,acylation and Wittig cyclization reaction of optically active material(3R,4R)...A compound ethyl(5S,6R)-2-(4-methylphenyl)-6-[(1R)-tert-butyldimethylsilyloxyethy]-penem-3-carboxylate was synthesized through displacement,acylation and Wittig cyclization reaction of optically active material(3R,4R)-3-[(1R)-tert-butyldimethylsilyloxyethyl]-4-acetoxy-2-azetidi-none(4AA)upon thionocarboxlic acid.The intermediates and the target product were characterized by 1HNMR,IR,elementary analysis and MS.展开更多
文摘2-氟-5-[(4-氧代-3,4-二氢二氮杂萘-1-基)甲基]苯甲酸是合成奥拉帕尼的关键中间体。以邻羧基苯甲醛为原料,与亚磷酸二甲酯反应得到磷叶立德,再与2-氟-5-甲酰基苯甲酸进行WittigHorner反应、环合反应得到目标化合物,并对各步反应条件进行了优化,三步反应总收率70.9%。目标化合物经(1 H NMR)和(MS)确证结构。
文摘A compound ethyl(5S,6R)-2-(4-methylphenyl)-6-[(1R)-tert-butyldimethylsilyloxyethy]-penem-3-carboxylate was synthesized through displacement,acylation and Wittig cyclization reaction of optically active material(3R,4R)-3-[(1R)-tert-butyldimethylsilyloxyethyl]-4-acetoxy-2-azetidi-none(4AA)upon thionocarboxlic acid.The intermediates and the target product were characterized by 1HNMR,IR,elementary analysis and MS.
