Bis (trimethylsilyl) amino sodium tetrahydrofuran solution is a strong alkaline catalyst used in organic synthesis. The synthesis of drug Mitiglunde intermediates using bis (trimethylsilyl) amino sodium tetrahydrofuran solution has achieved satisfactory results. The usual preparation method is to reflux hexamethyldisilane amine and sodium hydride in anhydrous tetrahydrofuran for a long time.
Application 1
CN201110457606.4 provides a preparation method for fosapitam dimethylglucosamine. In the presence of bis (trimethylsilyl) amino sodium, the method involves the condensation reaction of arepidan with tetrabenzyl pyrophosphate in tetrahydrofuran to obtain bis O-phenylphosphate, which is then heated with methanol to obtain mono O-phenylphosphate. Finally, fosapitam dimethylglucosamine is obtained through hydrogenation reaction. The method of the present invention has the advantages of simple operation, mild conditions, low cost, high yield, suitability for industrial production, and significant application value.
Application 2
CN201810842737.6 discloses a preparation method for phosphine chiral center sodium salt. The method first slowly drips Grignard reagent into a chiral phosphonate solution under nitrogen protection and -80 ℃, reacts overnight, adds a saturated ammonium chloride solution, and reacts to obtain a phosphonic chiral center compound. Then, under nitrogen protection, slowly drips equimolar bis (trimethylsilyl) amino sodium into a tetrahydrofuran solution of the phosphonic chiral center compound, and reacts overnight to obtain phosphonic chiral center sodium salt. The method of the present invention significantly shortens the reaction time, requiring only one reaction with the format reagent, resulting in a chiral compound with an ee value of over 90%, greatly improving the selectivity of phosphine chiral center compounds. At the same time, it can react with nucleophilic reagents to continue functionalization, and the prepared phosphine chiral center sodium salt has good stability, with a storage time of up to 30 days at room temperature.