Patent ID: 7214818
Filing Date: 2007-05-08
Classification: A61P,C07F

Abstract:
1. A process for the preparation of 3-(N-methyl-N-pentyl)amino-1-hydroxypropane-1,1-diphosphonic acid, monosodium salt, monohydrate of the formula I said process comprising: (a) condensing N-pentylamine with benzaldehyde to produce the N-benzylidene-N-pentylamine of formula II (b) transforming the N-benzylidene-N-pentylamine into N-methyl-N-pentylamine by reacting the N-benzylidene-N-pentylamine with a methylating agent (c) reacting the N-methyl-N-pentylamine with methyl acrylate to form N-methyl-N-pentyl-β-alanine methylester of the formula III (d) converting the N-methyl-N-pentyl-□-alanine methyl ester to a compound of formula IV wherein X is a halogen, and (e) bisphosphorylating the compound of formula IV by reacting the compound of formula IV with phosphoryl chloride and phosphorous acid subsequently forming the monosodium salt, monohydrate.