Enzymatic approach toward the synthesis of isotopically labeled (R)-9-(2-hydroxypropyl)adenine

Rivera, N. R., Moore, J., Schenk, D. J., Wang, H., Hesk, D., & Mergelsberg, I. (2016). Enzymatic approach toward the synthesis of isotopically labeled (R)-9-(2-hydroxypropyl)adenine. Tetrahedron Letters, 57(10), 1090-1092. https://doi.org/10.1016/j.tetlet.2016.01.087

Abstract

Isotopically labeled compounds have numerous applications in drug discovery and development. (R)-9-(2-Hydroxypropyl)adenine 1 is an important intermediate in the synthesis of various acyclic nucleoside phosphonates including tenofovir. We have developed a short synthetic method to prepare deuterium and tritium labeled 1 using a ketoreductase enzyme catalyzed reduction as the key step to introduce the label in a highly efficient and enantioselective way. (C) 2016 Elsevier Ltd. All rights reserved.

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