申请人:SmithKline Corporation
公开号:US03976695A1
公开(公告)日:1976-08-24
Halogen substituted .alpha.-(aminoalkyl)-3,4-dihydroxybenzyl alcohols having .beta.-adrenergic stimulant activity, particularly as selective bronchodilators. The .alpha.-aminomethyl derivatives are prepared by the condensation of an appropriately substituted styrene oxide with a primary amine followed by removal of the ether protective group(s). The .alpha.-aminoethyl or .alpha.-aminopropyl derivatives are prepared by the condensation of an appropriately substituted .alpha.-bromoalkyl phenyl ketone with an N-benzyl secondary amine followed by reduction of the ketone moiety and removal of the ether protective group(s).
具有β-肾上腺素激动剂活性的卤代α-(氨基烷基)-3,4-二羟基苯甲醇,特别是作为选择性支气管扩张剂。α-氨甲基衍生物通过适当取代的苯乙烯环氧化物与一级胺缩合制备,随后去除醚保护基。α-氨乙基或α-氨丙基衍生物通过适当取代的α-溴烷基苯酮与N-苄基二级胺缩合制备,随后还原酮基团并去除醚保护基。