Beta <sub> 2 </ Sub> - Adrenergic Receptor Agonist Phenylethanolamine Compounds Synthesis And Screening

In this paper, the pathogenesis of asthma was described concisely, the structure of β₂-adrenoceptor and the action mechanism of β₂-adrenoceptor agonist were introduced systematically at the molecular level, at the same time, the development and structure-activity relationship of β₂-adrenoceptor were reviewed. On the basis of structure-activity relationship of β₂- adrenoceptor agonist, twenty derivatives of phenylethanolamines were designed and synthesized on principle of isosterism, with considering the high efficiency, high selectivity and speciality of structure of mabuterol and SPFF. The structures of ZHY-13 to ZHY-20 were 1-phenyl-2-amino-ethanol hydrochlorides, which were obtained by the method of first amination and then reduction, but the structures of ZHY-01 to ZHY-12 were 2-phenyl-2-amino- ethanol hydrochlorides, which were obtained by another method of first reduction and then amination. ZHY-18,ZHY-19 and ZHY-20 were the isomeric compounds of ZHY-01, ZHY-03 and ZHY-06 respectively. The structures of the compounds were discussed from the mechanism and confirmed by their spectrum. And all compounds were identified by IR, ¹H-NMR and MS. Primary pharmacological tests showed that all compounds except for ZHY-05 had relaxing activity on the contracting bronchial smooth muscle of guinea-pigs induced by histamine.Moreover, CMPP resin was selected to study the connection, bromination, reduction and cleavage reactions for achieving the method of solid phase organic synthesis of phenylethanolamines.