abstract |
A pentasaccharide tuning for the preparation of synthetic heparinoids, said tuning being of General Formula I, General Formula I (EDCBA block) in which the configuration of the monosaccharide units and the stereochemistry of the internal junctions is defined as D-gluco-alpha- 1,4-D-glucurono-beta-1,4-D-Gluco-alfa-1,4-L-idurono-beta-1,4-D-gluco, and the substituents are defined as; X1 is selected from the group consisting of hydroxy, alkenyloxy, alkoxy, aryloxy, benzyloxy, substituted benzyloxy; thioalkyl, thioaryl, halogen, imidoyl, leaving groups of the phosphate type and related phosphate ester, a tbutyldiphenylsilyloxy or another substituted silyloxy protecting group of this type; a lipoamino acid or other suitable group of this type for conjugation in administration systems or solid supports; and the stereochemistry can be alpha or beta. |