| 摘要 |
A process for the preparation of a class of phenylalanine enamide derivatives is described formula (1) wherein: Aris an optionally substituted aromatic or heteroaromatic group; Lis a linker group selected from -N(R)- [where Ris a hydrogen atom or an optionally substituted straight or branched Calkyl group], -CON(R)-, or -S(O)N(R)-; Ris a carboxylic acid (-COH) or a derivative or biostere thereof; Ris a hydrogen atom or a Calkyl group; R, Rand Rwhich may be the same or different is each an atom or group –L(Alk)(R); and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Qis a group -N(R)H; and the salts, solvates, hydrates and N-oxides thereof; with a compound ArW wherein W is a group selected from X(wherein Xis a leaving atom or group), -COX(wherein Xis a halogen atom or a -OH group) or –SOX(in which Xis a halogen atom). |
