Improvement of synthetic technology of valganciclovir hydrochloride
Objective To improve the synthesis process of valganciclovir hydrochloride.Methods Valganciclovir hydrochloride was synthesized from ganciclovir by protection with acetyl to give O-monoacylganciclovir,which was subjected to condensation with Cbz-L-valine and deacetylated hydrochloride to obtain ganciclovir-Cbz-L-monovaline ester.After ganciclovir-Cbz-L-monovaline was acidified,hydrogenation of debenzyloxycarbonyl in a continuous flow reactor was catalyzed to obtain valganciclovir hydrochloride crude product,and the crude product was recrystallized in isopropanol/water(2∶1)to obtain valganciclovir hydrochloride.Result The improved process made the operation more convenient and safe,enabling long-term stable and safe continuous production and post-treatment.The yield and purity of target product 1 had been improved,with a total yield of 48.8％and a purity of 99.4％.Conclusion This research provided a relatively new method for the synthesis of valganciclovir hydrochloride,reducing production costs.
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