申请人:Cassella Farbwerke Mainkur Aktiengesellschaft
公开号:US03969363A1
公开(公告)日:1976-07-13
The present invention relates to new pharmacologically valuable derivatives of 1-phenoxy-3-amino-propan-2-ol having the formula ##EQU1## and the aldehyde condensation products and acid addition salts thereof wherein X is selected from the group consisting of ##EQU2## wherein the phenyl ring I may have attached to it up to three similar or different substituents selected from the group consisting of alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, alkoxy, alkenyloxy, alkinyloxy, benzyloxy, phenyl, halogen and --NR.sub.1 R.sub.2, wherein R.sub.1 is selected from alkyl and acyl, and R.sub.2 is selected from hydrogen and alkyl and n is 1, 2 or 3; and to the production thereof by a method selected from (A) reacting 1-phenoxy-3-amino-propan-2-ol having the formula ##EQU3## with a compound having the formula Y-X, wherein X has the above defined meaning and Y is selected from halogen, --OH, --OK or --ONa; (B) reacting a compound of the formula ##EQU4## with a compound of the formula H.sub.2 N--X, wherein X has the above-defined meaning and Z is selected from ##EQU5## and ##EQU6## (C) reacting a phenol ##EQU7## with Z--CH.sub.2 --NH--X, wherein X and Z have the meaning defined above.
本发明涉及1-苯氧基-3-氨基-丙烷-2-醇的新的药理学有价值的衍生物,其化学式为##EQU1##以及其醛缩合物和酸加成盐,其中X选自以下组中的一种##EQU2##其中苯环I可能连接有最多三个相似或不同的取代基,所述取代基选自烷基,烯基,炔基,环烷基,环烯基,烷氧基,烯氧基,炔氧基,苄氧基,苯基,卤素和--NR.sub.1 R.sub.2,其中R.sub.1选自烷基和酰基,R.sub.2选自氢和烷基,n为1、2或3;以及通过以下方法之一制备它们的方法:(A)反应具有以下式子的1-苯氧基-3-氨基-丙烷-2-醇与具有以下式子的化合物Y-X反应,其中X具有上述定义的含义,Y选自卤素,--OH,--OK或--ONa;(B)反应具有以下式子的化合物##EQU4##与具有以下式子的化合物H.sub.2 N--X反应,其中X具有上述定义的含义,Z选自##EQU5##和##EQU6##(C)反应苯酚##EQU7##与Z--CH.sub.2--NH--X反应,其中X和Z具有上述定义的含义。