Efficient Synthesis of Deuterium-Labelled Ganciclovir-d5 and Its Prodrug Valganciclovir-d5

An efficient protocol has been developed for the synthesis of deuterium labeled ganciclovir- d 5 , a potent anti-cytomegalovirus agent and its prodrug, valganciclovir- d 5 , by using inexpensive and commercially available glycerol- d 5 reagent. Structure and purity of the synthesized compounds are c...

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Bibliographic Details
Published in:Russian journal of general chemistry 2022, Vol.92 (4), p.739-742
Main Authors: Parameshwar, R., Durgaprasad, K., Prathap, M.
Format: Article
Language:English
Subjects:
Chemical synthesis
Chemistry
Chemistry and Materials Science
Chemistry/Food Science
Deuterium
Glycerol
NMR
Nuclear magnetic resonance
Reagents
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Summary:An efficient protocol has been developed for the synthesis of deuterium labeled ganciclovir- d 5 , a potent anti-cytomegalovirus agent and its prodrug, valganciclovir- d 5 , by using inexpensive and commercially available glycerol- d 5 reagent. Structure and purity of the synthesized compounds are confirmed by 1 H NMR and MS spectral data. The deuterium incorporation in ganciclovir- d 5 and its prodrug was >98% which resembles the reported earlier deuterium abundance in the labeled starting material (glycerol- d 5 , >98% atom D). The results indicate that there is no loss of deuterium by exchange in the course of synthesis. Hence, these molecules can be used as standards in bio-analytical studies.
ISSN:1070-3632
1608-3350
DOI:10.1134/S1070363222040168