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CN102212083A d4T-5′-氢亚磷酸薄荷醇酯及其制备方法和应用 无效 - 驳回

d4T-5′-氢亚磷酸薄荷醇酯及其制备方法和应用
摘要：
d4T-5′-氢亚磷酸薄荷醇酯及其制备方法和应用。涉及核苷氢亚磷酸酯，提供d4T-5′-氢亚磷酸薄荷醇酯及其制备方法和应用。d4T-5′-氢亚磷酸薄荷醇酯为白色固体，化学名为2′，3′-双脱氢-2′，3′双脱氧胸苷-5′-氢亚磷酸薄荷醇酯，分子式为C20H31N2O6P，相对分子质量为426。用特戊酰氯作为为缩合剂，使d4T和薄荷醇在碱性溶剂里，先后与亚磷酸的两个羟基缩合，用一锅法合成d4T-5′-氢亚磷酸薄荷醇酯。制备的d4T-5′-氢亚磷酸薄荷醇酯可抑制逆转录酶的活性，作为核苷逆转录酶抑制剂，在制备抗艾滋病药物中具有广泛的应用。合成原料易得反应时间短，步骤少，条件温和，产率达到69％。
摘要（英）：

The invention discloses d4T-5'-hydro-ortho-phosphorous acid menthol ester and a preparation method and application thereof, relates to nucleoside hydro-ortho-phosphorous acid ester and provides d4T-5'-hydro-ortho-phosphorous acid menthol ester and a preparation method and application thereof. The d4T-5'-hydro-ortho-phosphorous acid menthol ester is a white solid and has the chemical name being 2',3'-bisdehydro-2',3'bideoxythymidine-5'-hydro-ortho-phosphorous acid menthol ester, the molecular formula being C20H32N2O6P, and the relative molecular mass being 426. The preparation method comprises the following steps of: condensing d4T and menthol with two hydroxyl groups of ortho-phosphorous acid in sequence in a basic solvent by taking pivaloyl chlorine as a condensing agent; and synthesizing d4T-5'-hydro-ortho-phosphorous acid menthol ester in a one-kettle way. The prepared d4T-5'-hydro-ortho-phosphorous acid menthol ester can restrain the activity of reverse transcriptase, is taken as an inhibitor of nucleoside reversed transcriptive enzyme, and is widely applied to the preparation of an anti-acquired immune deficiency syndrome medicament. The method has the advantages of readily available synthesis raw materials, short reaction time, less steps, mild condition and yield up to 69 percent.

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