Preparation of acylaminomethanephosphonic acids and...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/30 (2006.01) C07F 9/38 (2006.01)

Patent

CA 2089652

Acylaminomethanephosphinic acids, and a process for the preparation of acylaminomethanephosphonic acids and acylaminomethylphosphinic acids Acylaminomethanephosphonic acid and acylaminomethyl- phosphinic acids of the formula I, R2 - CO - NH - CH2 - P(O)(OH)R1 (I) in which R1 is hydroxyl, C1-C4-alkyl or phenyl and R2 is H, C1-C5-alkyl, benzyl or phenyl, unsubstituted or sub- stituted by one or more radicals from the group compris- ing C1-C4-alkyl, C1-C4-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 R2 - CO - NH - CH2 - OH (II) with compounds of the formula III, H - p(O)(OH)R1 (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 (T) where R1 is other than hydroxyl, are novel.

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