申请人:Pfizer Inc.
公开号:US04517379A1
公开(公告)日:1985-05-14
Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is CH.sub.2 OH or CH.sub.2 OCH.sub.3 ; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, F.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2, C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.9 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms and the sum of the carbon atoms in R.sup.7, R.sup.8 and R.sup.9 is not greater than six, m and q are the same or different and each have the values previously defined for m; ##STR4## where each of R.sup.12 and R.sup.13 are methyl or ethyl, or R.sup.12 is hydrogen and R.sup.13 is alkyl having from one to four carbon atoms, Z is O or NH and t is 1 or 2, ##STR5## where w is 1-4, R.sup.14 and R.sup.16 are each alkyl having from one to four carbon atoms, R.sup.15 is H, OH, methyl or ethyl and the sum of the carbon atoms in R.sup.14, R.sup.15 and R.sup.16 is not greater than six and when both of R.sup.14 and R.sup.15 are alkyl they are methyl or ethyl, and ##STR6## where R.sup.17 and R.sup.19 are alkyl having from one to four carbon atoms, R.sup.18 and R.sup.20 are H or alkyl having one to two carbon atoms, A is OH and B is H, OH or CH.sub.3 and taken together A and B are ##STR7## where the sum of the carbon atoms in R.sup.17, R.sup.18, R.sup.19 and R.sup.20 is not greater than six and when both of R.sup.17 and R.sup.18 or R.sup.19 and R.sup.20 are alkyl they are methyl or ethyl; said amides are potent sweeteners having advantages over the prior art, edible compositions containing them, methods for their use in edible compositions and novel amide intermediates useful in their production.
L-天冬氨酸-D-氨基酸二肽的酰胺,其化学式为##STR1##以及其生理可接受的阳离子和酸性加成盐,其中R.sup.a是CH.sub.2 OH或CH.sub.2 OCH.sub.3; R是从羟基萜、二异丙基甲基、d-甲基-t-叔丁基甲基、d-乙基-t-叔丁基甲基、二-叔丁基甲基、2-甲硫基-2,4-二甲基戊烷-3-基,##STR2##其中R.sup.3、F.sup.4、R.sup.5、R.sup.6中至少有一个是1-4个碳原子的烷基,其余为氢或1-4个碳原子的烷基,X为O、S、SO、SO.sub.2、C.dbd.O或CHOH; m为0或1-4,n和p各自为0、1、2或3,其中n+p之和不大于3,R.sup.3、R.sup.4、R.sup.5和R.sup.6中碳原子的总和不大于6,当R.sup.3和R.sup.4或R.sup.5和R.sup.6都是烷基时,它们是甲基或乙基,##STR3##其中R.sup.7、R.sup.8、R.sup.9中的一个是1-4个碳原子的烷基,其余为氢或1-4个碳原子的烷基,R.sup.7、R.sup.8和R.sup.9中碳原子的总和不大于6,m和q相同或不同,其值与m的定义相同; ##STR4##其中R.sup.12和R.sup.13都是甲基或乙基,或R.sup.12是氢,R.sup.13是1-4个碳原子的烷基,Z为O或NH,t为1或2,##STR5##其中w为1-4,R.sup.14和R.sup.16都是1-4个碳原子的烷基,R.sup.15为H、OH、甲基或乙基,R.sup.14、R.sup.15和R.sup.16中碳原子的总和不大于6,当R.sup.14和R.sup.15都是烷基时,它们是甲基或乙基,以及##STR6##其中R.sup.17和R.sup.19是1-4个碳原子的烷基,R.sup.18和R.sup.20是氢或1-2个碳原子的烷基,A为OH,B为H、OH或CH.sub.3,且A和B在一起为##STR7##其中R.sup.17、R.sup.18、R.sup.19和R.sup.20中碳原子的总和不大于6,当R.sup.17和R.sup.18或R.sup.19和R.sup.20都是烷基时,它们是甲基或乙基; 这些酰胺是具有优于现有技术的优点的强效甜味剂,可食用组合物包含它们,在可食用组合物中使用它们的方法以及在它们的生产中有用的新型酰胺中间体。