PROCESS FOR THE ENANTIOSELECTIVE SEPARATION OF AMINO ACIDS USING CHIRAL POLYSTYRENE MICROSPHERES

    公开(公告)号:US20250050312A1

    公开(公告)日:2025-02-13

    申请号:US18719595

    申请日:2022-12-13

    Abstract: The present invention relates to an enantioselective separation of racemic mixtures of amino acids like alanine and leucine using chiral polystyrene microspheres. It provides a simple and efficient separation process by using cost-effective commodity polymer like polystyrene after simple post polymer modifications which involves simple filtration without using any high end chromatographic instrument. The present process provides the preparation of chiral modified protected or deprotected polystyrene powder. The present invention provides a process of preparing the modified polystyrene to form the deprotected polystyrene along with the process of preparation of the modified poly styrene compound in fiber form or microspheres form wherein the change in the morphology is observed from irregular to fibrous upon deprotecting the protected polymer. This process achieves high separation efficiency and % Enantiomeric excess values (% ee) value.

    PROCESS FOR THE PREPARATION OF 2,7-DIHYDROXY-9-FLUORENONE USEFUL FOR THE SYNTHESIS OF TILORONE AND ITS SALTS

    公开(公告)号:US20240409495A1

    公开(公告)日:2024-12-12

    申请号:US18702639

    申请日:2022-10-19

    Abstract: Methods involving preparation of building blocks of 2,7-dihydroxy-9-fluorenone toward the synthesis of tilorone dihydrochloride salt and other salts (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate) of tilorone, and an efficient, safe, cost effective method for the preparation of 2,7-bis-[2-(diethylamino)ethoxy]-fluorenone-9 and its various salts are developed. The methods involve oxygenation of fluorene, nitration of fluorenone, followed by reduction and diazotization toward the formation of 2,7-dihydroxy-9-fluorenone, which is the key intermediate for the formation of 2,7-bis-[2-(diethylamino)ethoxy]-9-fluorenone-dihydrochloride (Tilorone dihydrochloride) and other tilorone salts. The synthesis method has relatively simple operation, mild reaction conditions, high yield, and simple process with yields of 80-97%. Subsequent product purification of this method uses filtration and crystallization methods, avoiding the existing methods of column chromatography. Therefore, the research of its synthetic method being with a wide range of applications from the drug development and material synthesis point of view.

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