PROCESS FOR THE PREPARATION OF PHENYLALANINE ENAMIDE DERIVATIVES

摘要

A process for the preparation of a class of phenylalanine enamide derivatives is described: wherein: Ar¹ is an optionally substituted aromatic or heteroaromatic group; L² is a linker group selected from -N(R⁴)- [where R⁴ is a hydrogen atom or an optionally substituted straight or branched C_1-6alkyl group], -CON(R⁴)-, or -S(O)₂N(R⁴)-; R¹ is a carboxylic acid (-CO₂H) or a derivative or biostere thereof; R² is a hydrogen atom or a C_1-6alkyl group; R^x, R^y and R^z which may be the same or different is each an atom or group -L¹(Alk¹)_n(R³)_v; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Q^a is a group -N(R⁴)H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar¹W wherein W is a group selected from X¹(wherein X¹ is a leaving atom or group), -COX² (wherein X² is a halogen atom or a -OH group) or -SO₂X³ (in which X³ is a halogen atom).