PROCESS FOR PRODUCING ALPHA-AMINOPHOSPHONIC ACIDS AND THEIR PEPTIDES AND COMPOUNDS THUS OBTAINED

摘要

The present invention provides a process for the production of physiologically-useful alpha -aminophosphonic acids and peptide derivatives of the formula: I wherein R and R1 may be the same or different and each can be hydrogen, deuterium or an optionally substituted lower alkyl group, lower alkenyl, lower alkynyl, cycloalkyl, aryl or heterocyclic radical containing one or more oxygen, nitrogen or sulphur atoms and which may be fused to an aromatic ring, a lower alkyl group substituted by a cycloalkyl radical, a lower alkyl group substituted by an aryl radical, a lower alkyl group substituted by a heterocyclic radical as defined above or R and R1 together form a polymethylene chain optionally interrupted by an oxygen, nitrogen or sulphur atom, or R1 represents, together with the C(R)-N< residue to which it is attached, the atoms required to complete a heterocyclic radical; and R2 can be hydrogen, optionally substituted lower alkyl, cycloalkyl, aryl or lower alkyl substituted by a cycloalkyl radical, lower alkyl substituted by a heterocyclic radical containing one or more nitrogen atoms; by a heterocyclic radical containing one or more nitrogen atoms, or R2 together with the C(H)-N residue to which it is attached, may represent the atoms required to complete a heterocyclic radical; and n is 0, 1, 2, 3 or 4; comprising oxidizing, using an oxidizing agent, a compound having the formula: II wherein R, R1, R2 and n have their previous significance, and Z is H or a protecting group usually used for an amino group; and then removing any protecting group.