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

In this paper, the pathogenesis of the asthma was described concisely, the structure of β₂－adrenoceptor and the mechanism of action of β₂－adrenoceptor agonist were introduced systematically on the molecular level, the development and structure-activity relationship of β₂－adrenoceptor were reviewed. On the basis of structure-activity relationship of β₂－adrenoceptor agonist, seventeen derivatives of phenylethanolamines were designed and synthesized by the principle of isosterism, under considering the high efficiency, high selectivity and speciality of structure of mabuterol. The structures of ZL-001 to ZL-015 were 1-phenyl-2-amino-ethanol hydrochlorides, which were obtained by the method of first animation and then reduction, but the structures of ZL-016 and ZL-017 were 2-phenyl-2-amino-ethanol hydrochlorides, which were obtained by another method of first reduction and then animation. ZL-001 and ZL-003 are the isomeric compounds of ZL-016 and ZL-017 respectively. The structures of the compounds were discussed from the mechanism and the differences of spectrum. And all compounds were identified by IR, 'H-NMR and MS. Primarypharmacological tests showed that nine target compounds(ZL-001 004, 006,007, 008, 009, 010, 011 , 016)had moderate relaxing activity on the contractingbronchial smooth muscle of guinea-pigs induced by histamine.Otherwise, CMPP resin was selected to study the connection, bromination, reduction and cleavage reactions for achieving the method of solid phase synthesis of phenylethanolamines.