申请人:A. H. Robins Company, Incorporated
公开号:US04806555A1
公开(公告)日:1989-02-21
Novel 1-aryloxy-4-amino-2-butanols of the formula ArO--CH.sub.2 --CHOH--CH.sub.2 --CH.sub.2 --NR.sup.1 R.sup.2 wherein Ar is 1-naphthyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R.sup.1 is lower alkyl, phenyl, phenylalkyl, 2-hydroxymethyl-2-propyl, adamantyl or lower-cycloalkyl, R.sup.2 is hydrogen or lower alkyl, wherein R.sup.1 and R.sup.2 together with the adjacent nitrogen from a heterocyclic residue and the pharmaceutically acceptable acid addition salts thereof having local anesthetic, beta-adrenergic blocking, antihypertensive and antiarrhythmic properties are disclosed. The compounds are prepared by reacting novel 1-aryloxy-4-chloro-2-butanols with amines. Methods for the preparation of the novel 1-aryloxy-4-chloro-2-butanol intermediates are also disclosed.
化合物的名称为Novel 1-aryloxy-4-amino-2-butanols,化学式为ArO--CH.sub.2 --CHOH--CH.sub.2 --CH.sub.2 --NR.sup.1 R.sup.2,其中Ar可以是1-萘基、2-萘基、茚-4(或5-)基、3-(或5-)氯基-2-吡啶基、苯基、单取代苯基或二取代苯基,R.sup.1可以是较低的烷基、苯基、苯基烷基、2-羟甲基-2-丙基、金刚烷基或较低的环烷基,R.sup.2可以是氢或较低的烷基。这些化合物与相邻氮原子组成杂环残基,并且它们的药物可接受的酸盐具有局部麻醉、β-肾上腺素受体阻滞、降压和抗心律失常的性质。这些化合物是通过将新型的1-芳氧基-4-氯-2-丁醇与胺反应制备而成的。此外,还公开了制备新型1-芳氧基-4-氯-2-丁醇中间体的方法。