Synthesis And Inhibition Of Gastric Juice Acid Of Roxatidine Acetate And Its Analogues

The pathogenesis of digestible ulcer and the cure function for H₂-receptor antagonists were reviewed in this paper. The pharmacological peculiarity of the fourth histamine H₂-Receptor antagonists(Roxatidine acetate) is described in much detail. The four-step synthetic process of roxatidine acetate was investigated and carried out. Total yield ranged to 29%. The final product was identified by comparing to the spectrum data in literature. Seven primary amines (cyclopentamine, cyclohexylamine, methylamine, n-butylamine, isopropylamine, isobutylamine, tert-butyl amine) were selected to design and synthesize a series of phenoxypropylamide on the basic theory of the principle of bioisosterism. Their chemical structures were identified by ¹H-NMR and MS. All of them were not reported in CA. The primary pharmacological tests showed that two of them had higher percent of inhibition of gastric juice acid output. Further study will be done in the future.