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PHOSPHORIC ACID ESTER COMPOUND OF HYDROXY ACID SUBSTITUTED PHENYL ESTER, SYNTHESIS METHOD AND MEDICAL USE THEREOF

机译:羟基取代苯甲酸酯的磷酸酯化合物,合成方法及其医学用途

摘要

Phosphate ester compound of hydroxy acid substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), in which Y = C 1-4 straight carbon chain, M 1 and/or M 2 = H, alkali metal ion, protonated amine or protonated amino acid. The compound has good water solubility and high stability in its aqueous solution, and it can release 2, 6-diisopropylphenol rapidly under the action of enzymes in vivo, which has the effects of sedation, hypnosis and/or anesthesia. By protecting hydroxyl of 2, 6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2, 6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis and/or anesthesia.
机译:提供了羟基取代苯基酯的磷酸酯化合物,其制备方法和医学用途。标题化合物如式(I)所示,其中Y = C 1-4直碳链,M 1和/或M 2 = H,碱金属离子,质子化胺或质子化氨基酸。该化合物在水中具有良好的水溶性和高稳定性,在体内酶的作用下可以迅速释放出2,6-二异丙基苯酚,具有镇静,催眠和/或麻醉作用。通过保护式(I)的化合物中的2,6-二异丙基苯酚的羟基,降低了2,6-二异丙基苯酚的首过代谢活性,使得合成的化合物可用于镇静,催眠和/或麻醉。

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