盐酸罗沙替丁乙酸酯的合成

Synthesis of Roxatidine Acetate Hydrochloride

间羟基苯甲醛和哌啶缩合得到的3-(1-哌啶甲基)苯酚,与3-氯丙胺在DMF中于90～95℃直接缩合制得3-(3-(1-哌啶基甲基)苯氧基)丙胺,再依次和氯乙酰氯和乙酸钾经缩合反应得到抗溃疡药盐酸罗沙替丁乙酸酯,总收率59%。

Roxatidine was synthesized from 3-（piperidin-l-ylmethyl）phenol by condensation with 3-chloropropylamine in DMF at 90-95℃ to give 3- [ （3-piperidin-1-ylmethyl） phenoxy] propylamine followed by successive reactions with chloroacetyl chloride and potassium acetate in 59 % overall yield.