Article
A Practical and Scalable Synthesis of GTx-134, an IGF-1R Inhibitor
Yahu A. Liu,
Vlad E. Gregor,
Corresponding Author
Yahu A. Liu
ChemBridge Research Laboratories, Inc., San Diego, California, 92127 USA
E-mail: [email protected]Search for more papers by this authorVlad E. Gregor
ChemBridge Research Laboratories, Inc., San Diego, California, 92127 USA
Search for more papers by this authorYahu A. Liu,
Vlad E. Gregor,
Corresponding Author
Yahu A. Liu
ChemBridge Research Laboratories, Inc., San Diego, California, 92127 USA
E-mail: [email protected]Search for more papers by this authorVlad E. Gregor
ChemBridge Research Laboratories, Inc., San Diego, California, 92127 USA
Search for more papers by this authorFirst published: 04 June 2015
This work was dedicated in memory of Dr. Vlad E. Gregor (1954–2010) who made great contributions to medicinal chemistry and drug discovery.
Abstract
A practical and scalable synthesis of GTx-134, a novel small-molecule inhibitor of insulin-like growth factor 1 receptor showing antitumor activity in preclinical models of multiple myeloma, is reported.
References and Notes
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- 204-Chloro-2-methoxy-1,2-dihydropyridine-3-carbaldehyde (16), the lowest price in June, 2014: $65.0/mmol ($380/g) (Broadpharm, San Diego, CA, 92121); 4-Iodo-2-methoxy-1,2-dihydropyridine-3-carbaldehyde (7), the lowest price in November, 2014: $65.8/mmol ($250/g) (Key Organics, Camelford, Cornwall, PL32 9RA, UK).
