Premium
An innovative and efficient synthesis of stable isotope labelled 1‐methyl‐5‐(4,4,5,5‐tetramethyl‐1,3,2‐dioxaborolan‐2‐yl)‐1H‐pyrazole via [ 13 C 4 2 H 3 ] N ‐methylpyrazole
Author(s) -
Manning Calvin,
Athlan Audrey,
Badman Geoff
Publication year - 2012
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.2971
Subject(s) - chemistry , malonate , diethyl malonate , pyrazole , stable isotope ratio , isotope , combinatorial chemistry , medicinal chemistry , stereochemistry , organic chemistry , catalysis , physics , quantum mechanics
In support of a programme to develop a treatment for cancer, a stable isotope labelled version of the drug candidate was required. The key labelled intermediate was [ 13 C 4 2 H 3 ] N ‐methylpyrazole prepared by a novel bisacetal cyclisation. This was prepared from commercially available diethyl [ 13 C 3 ] malonate and [ 13 C 2 H 3 ] iodomethane. Copyright © 2012 John Wiley & Sons, Ltd.