一种新型磷酰胺吗啉代寡鸟苷酸单体的合成及工艺优化.

A synthesis route of a novel phosphoramide morpholinoline-oligoguanylate monomer using guanosine as raw material was developed.Based on the protection of the amino group on the base and 5’-OH in ribose, the ribose ring is converted into a morpholine ring to obtain the protected morpholine guanosine.A triphenylmethylation reaction was carried out on the morpholine ring and purine 6-O position was modified using the Mitsunobu reaction.N,N-dimethylaminophosphorylation reaction is performed on the deprotected hydroxyl group to synthesize the target product.In this study, the conditions of the Mitsunobu reaction and phosphorylation reaction were optimized.Under optimized conditions, the total yield of the new synthetic route was 14.1%.The structure of intermediate products and target products were characterized by LC-MS, ¹H NMR and 31P NMR. [ABSTRACT FROM AUTHOR]