申请人:Hoechst Aktiengesellschaft
公开号:US05432291A1
公开(公告)日:1995-07-11
Acylaminomethanephosphinic acids, and a process for the preparation of acylaminomethanephosphonic acids and acylaminomethylphosphinic acids Acylaminomethanephosphonic acid and acylaminomethylphosphinic acids of the formula I, R.sup.2 --CO--NH--CH.sub.2 --P(O)(OH)R.sup.1 (I) in which R.sup.1 is hydroxyl, C.sub.1 -C.sub.4 -alkyl or phenyl and R.sup.2 is H, C.sub.1 -C.sub.6 -alkyl, benzyl or phenyl, unsubstituted or substituted by one or more radicals from the group comprising C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy and halogen, are valuable intermediates for the preparation of biologically active compounds. They can be prepared by reacting a compound of the formula II R.sup.2 --CO--NH--CH.sub.2 --OH (II) with compounds of the formula III, H--P(O)(OH)R.sup.1 (III) in the presence of an at least equimolar amount of acetic anhydride, based on the compound of the formula II. The compounds of the formula (I) where R.sup.1 is other than hydroxyl, are novel.
酰胺甲磷酸和酰胺甲基膦酸的制备方法酰胺甲磷酸和式I的酰胺甲基膦酸,R.sup.2--CO--NH--CH.sub.2--P(O)(OH)R.sup.1(I),其中R.sup.1为羟基、C.sub.1-C.sub.4-烷基或苯基,R.sup.2为H、C.sub.1-C.sub.6-烷基、苄基或苯基,未经取代或经由C.sub.1-C.sub.4-烷基、C.sub.1-C.sub.4-烷氧基和卤素等基团的取代,对于生物活性化合物的制备是有价值的中间体。它们可以通过将式II的化合物R.sup.2--CO--NH--CH.sub.2--OH(II)与式III的化合物H--P(O)(OH)R.sup.1(III)在存在至少等摩尔量的乙酸酐的情况下反应制备,基于式II的化合物。其中R.sup.1不为羟基的式(I)化合物是新颖的。