BioChem - DOS

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

Tetrahedron letters: the international organ for the rapid publication of preliminary communications in organic chemistry

Rivera, Nelo R.; Moore, Jeffrey; Schenk, David J.; Wang, Heather; Hesk, David; Mergelsberg, Ingrid

<P><B>Abstract</B></P> <P>Isotopically labeled compounds have numerous applications in drug discovery and development. (<I>R</I>)-9-(2-Hydroxypropyl)adenine <B>1</B> 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 <B>1</B> using a ketoreductase enzyme catalyzed reduction as the key step to introduce the label in a highly efficient and enantioselective way.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

2016

Elsevier

0040-4039

1873-3581

57

10

pp.1090-1092

10.1016/j.tetlet.2016.01.087

http://click.ndsl.kr/servlet/OpenAPIDetailView?keyValue=05787966&target=NART&cn=NART74971293

Ketoreductase; Stable isotope labeled (SIL); Deuterium; Tritium; Biocatalysis