| 摘要 |
<p>The sphingosine derivatives of the formula …<IMAGE>… which are described in European Patent Application No. 146,810 are prepared by D-galactose being protected in 4,6 position and oxidised to the corresponding D-threose protected in 2,4 position, an aliphatic chain (R<3>) being condensed onto the latter by Wittig reaction, the free hydroxyl group being converted into an azido group, and the protective group being eliminated, the resulting 2-azido-1,3-dihydroxy compound being selectively protected in 1 position and blocked in 3 position, the 1-hydroxy group being unblocked and the resulting compound or the abovementioned 2-azido-1,3-dihydroxy compound undergoing glycosidation with the O-trifluoro- or O-trichloroacetimidate or the 1-halogen derivative of a 2,3,4,6-O-tetraacyl-D-glucose, the acyl groups or these and the protective group in 3 position being eliminated, the azido being converted into an amino group and the amino compound being acylated with a fatty acid R<1>-OH. The process provides the compounds of the therapeutically more effective D series in relatively few stages without fractionation of diastereomers and in good yield.</p> |
