abstract |
REFERRING TO A PROCEDURE FOR THE PREPARATION OF A GLUTAMIC ACID DERIVATIVE OF FORMULA (I) WHICH CONSISTS OF: a) REACTING A COMPOUND OF FORMULA (VIII) WITH AN ORGANOMETHALLIC COMPOUND SUCH AS MAGNESIUM ISOPROPYL OR LITHIUM HYDROGEN DIISOPYL ZINC ISOPROPYL, TO GIVE A COMPOUND OF FORMULA (X) WHICH IS TREATED WITH SULFURIC ACID AND A CHLOROACETONITRILE TO GIVE A COMPOUND OF FORMULA (XIII); b) TREATING THE FORMULA COMPOUND (XIII) WITH A BASE AND / OR THIOUREA TO GIVE A FORMULA COMPOUND (XIV); c) TREATING THE COMPOUND OF FORMULA (XIV) WITH A COMPOUND SELECTED FROM (IV), (IVb) OR (II) TO GIVE A COMPOUND OF FORMULA (V), FROM WHICH THE PROTECTIVE GROUP IS REMOVED AND A COMPOUND OF FORMULA (VI) THAT WHEN TREATING IT WITH AN ACID CHLORIDE OF FORMULA R1C (= O) C1, IN THE PRESENCE OF A BASE, A COMPOUND OF FORMULA (VII) IS OBTAINED FROM WHICH THE PROTECTIVE GROUP IS REMOVED AND A COMPOUND OF FORMULA (I); WHERE R1 IS PHENYL, TRICYCLIC ARYL, BIPHENYL, AMONG OTHERS; R2 IS H, C1-C6 ALKYL, C2-C6 ALKENYL, AMONG OTHERS; PG1 IS A PROTECTIVE GROUP OF AMINE; PG2 IS A PROTECTIVE GROUP FOR CARBOXYL ACID; n IS AN INTEGER FROM 0 TO 4; R17 AND R18 ARE H, HALOGEN, CN, CF3, AMONG OTHERS. |