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Synthesis of [2‐ 14 C]‐2′‐deoxycytidine‐ 3 N‐cyanoborane
Author(s) -
Burnham Bruce S.,
Wyrick Steven D.,
Hall Iris H.,
Sood Anup,
Spielvogel Bernard F.
Publication year - 1991
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580290412
Subject(s) - chemistry , deoxycytidine , pyrimidine , boranes , stereochemistry , radiochemistry , boron , combinatorial chemistry , organic chemistry , cancer , medicine , gemcitabine
Synthetic nucleosides (e.g., 5‐fluorouracil, 6‐mercaptopurine) are used extensively as antineoplastic drugs. Recent research in boron chemistry has lead to the development of a series of amine‐boranes that possess significant antineoplastic activity. The agents may also be useful in boron neutron capture therapy (BNCT), therefore giving the compounds a dual mechanism of cytotoxic action. Herein is a report of the synthesis of one of the more active boronated nucleosides, 2′‐deoxycytidine‐ 3 N‐cyanoborane with a 14 C‐label in the 2‐position of the pyrimidine ring.