申请人:American Cyanamid Company
公开号:US04981989A1
公开(公告)日:1991-01-01
Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from one or more of: (a) C.sub.1 -C.sub.24 branched or straight chain alkyl; (b) C.sub.1 -C.sub.24 branched or straight chain alkoxy; (c) ##STR2## wherein n and m are integers from 0 to 25 and the sum of n and m is less than or equal to 25; phenyl; substituted phenyl wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, trifluoromethyl, phenyl, and substituted phenyl, phenoxy; and substituted phenoxy, wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, halogen, trifluoromethyl, phenyl and substituted phenyl; Q is selected from the group consisting of: ##STR3## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino and wherein R.sub.3 is C.sub.1 -C.sub.4 alkyl, with the proviso that when Q is ##STR4## then R.sub.1 is C.sub.1 -C.sub.4 branched or straight chain alkyl; T is a bivalent radical selected from the group consisting of --(CHR).sub.p -- and ##STR5## wherein p is an integer from 1 to 15, the moiety --(CHR).sub.p -- represents an alkylene chain substituted at any position with one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups, and the moiety ##STR6## is bound with the oxygen atom attached directly to the aromatic ring; and Z is ##STR7## wherein R.sub.2 is hydrogen or C.sub.1 -C.sub.4 branched or straight chain alkyl and q is an integer from 4 to 7; in either the racemic or optically active forms.
本文描述了具有以下公式的降压磷酸酯衍生物:##STR1##
其中X从以下一个或多个中选择:(a) C.sub.1-C.sub.24支链或直链烷基;(b) C.sub.1-C.sub.24支链或直链烷氧基;(c) ##STR2##
其中n和m是0到25的整数,并且n和m的和小于或等于25;苯基;取代苯基,其中取代基被选择自由基组,该自由基组由C.sub.1-C.sub.20支链或直链烷基,C.sub.1-C.sub.20支链或直链烷氧基,卤素,三氟甲基,苯基和取代苯基组成,苯氧基;和取代苯氧基,其中取代基被选择自由基组,该自由基组由C.sub.1-C.sub.20支链或直链烷基,卤素,三氟甲基,苯基和取代苯基组成;Q被选择自由基组,该自由基组由以下组成:##STR3##
其中R.sub.1被选择自由基组,该自由基组由氢,C.sub.1-C.sub.4支链或直链烷基,C.sub.1-C.sub.4支链或直链烷氧基和C.sub.1-C.sub.4支链或直链烷基胺组成,其中R.sub.3是C.sub.1-C.sub.4烷基,但是当Q是##STR4##时,R.sub.1是C.sub.1-C.sub.4支链或直链烷基;T是选择自由基组,该自由基组由以下组成:--(CHR).sub.p--和##STR5##
其中p是1到15的整数,基团--(CHR).sub.p--表示取代任何位置具有一个或多个C.sub.1-C.sub.10烷基或苯基的烷基链,基团##STR6##与直接连接到芳香环的氧原子相结合;Z是##STR7##
其中R.sub.2是氢或C.sub.1-C.sub.4支链或直链烷基,q是4到7的整数;可以是外消旋或光学活性形式。