Simple Preparation of Acyclic Adenylate and Its Inhibitory Activity of Protein Synthetase

病毒处理的干扰素细胞提取物中发现的2‘-5’寡腺苷(2-5A)是一种很强的蛋白合成酶抑制物。2-5A被认为激活核糖核酸酶L(核糖核酸酶L)裂解mRNA，从而抑制蛋白质合成酶。从那时起，野生型2-5A的制备一直被许多小组研究。然而，2-5A很容易被核酸酶切割成磷酸。半值期为2-3分钟。如果这一弱点被克服，2-5A将成为具有免疫激活剂的有效抗病毒药物的候选者。以1，3-二氧杂环己烷为原料，经一锅反应制得双-1，3-二氧杂环戊烷二核苷。3)低聚二氧杂环己烷与硫键取代制备低聚腺苷酸酯，但二氧杂环己烷和羟醛的中间体二恶戊烷尚未大规模分离。进一步的准备工作正在调查中。

2'-5' Oligo adenylate (2-5 A) found in the cell cultured extract from inferferon treated with virus is a strong inhibitor of protein synthetase. 2-5 A is considered to activate ribonuclease L (RNase L) to cleave m RNA resulting in inhibiting protein synthetase. Since then, preparation of wild type 2-5 A have been investigated by many group. However, 2-5 A is easily subject to cleavage of phosphate with nuclease. The half-value period has 2-3 minutes. If this weak point is overcome, 2-5 A will be a candidate of a potent anti-virus agent with immune activator. To prepare 2-5 A like acydlic oligoadenylate, the three following preparations were investigated.1) Adenyl phosphonate was successfully prepared from 1, 3-dioxolane.2) Dinucleosides were obtained from bis-1, 3-dioxolane by one-pot reaction.3) Preparation of oligoadenylate from oligodioxolane was examined by substitution of phosphonate with sulfur linkage, but the intermediate dioxolane from diol and hydroxyaldehyde has not been isolated in large scale. Further preparation is being investigated.