This invention relates to a method for preparing
sitagliptin phosphate to extend the lifespan of immobilized transaminases, belonging to the field of pharmaceutical synthesis technology. To address the problem of short lifespan of existing immobilized enzymes, this invention provides a method for preparing
sitagliptin phosphate to extend the lifespan of immobilized transaminases. The method includes, in the presence of immobilized transaminases, carrying out an enzymatic reaction of
sitagliptin precursor
ketone and
isopropylamine in a non-water-soluble
organic solvent. The reaction is terminated after the
raw material conversion rate is detected to be ≥75%, the immobilized transaminases are recovered, the filtrate is washed with water to remove
acetone, and an aqueous
phosphate solution is added to the filtrate for extraction. The aqueous phase is separated to obtain an aqueous
sitagliptin phosphate solution, and the
solvent is removed. The organic phase is washed with water and directly reused. This invention can significantly shorten the reaction time, reduce the
contact time of the immobilized transaminases in a high-concentration
acetone system, and avoid excessive soaking time, thereby extending the overall lifespan of the immobilized transaminases.