Microwave-assisted organic synthesis of a high-affinity pyrazolo-pyrimidinyl TSPO ligand

A microwave-assisted total synthesis of the high-affinity TSPO ligand, DPA-714, is reported. This protocol could enable high-throughput development of focused libraries of novel TSPO ligands. We herein report a dramatically improved total synthesis of the high-affinity translocator protein (TSPO) li...

Full description

Saved in:
Bibliographic Details
Published inTetrahedron letters Vol. 51; no. 35; pp. 4595 - 4598
Main Authors Tang, Dewei, Buck, Jason R., Hight, Matthew R., Manning, H. Charles
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 01.09.2010
Elsevier
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
LANTHANIDE CHELATE
PROTEIN 18 KDA
RADIOLIGAND
CANCER
PET
PERIPHERAL BENZODIAZEPINE-RECEPTOR
Online AccessGet full text

Cover

More Information
Summary:A microwave-assisted total synthesis of the high-affinity TSPO ligand, DPA-714, is reported. This protocol could enable high-throughput development of focused libraries of novel TSPO ligands. We herein report a dramatically improved total synthesis of the high-affinity translocator protein (TSPO) ligand DPA-714, featuring microwave-assisted organic synthesis (MAOS). Compared with previously described approaches, our novel MAOS method dramatically reduces overall reaction time without adversely effecting reaction yields. We envision that the described MAOS protocol may be suitably applied to high-throughput, diversity-oriented synthesis of novel compounds based on the pyrazolo-pyrimidinyl scaffold. Such an approach could accelerate the development of focused libraries of novel TSPO ligands with potential for future development as molecular imaging and therapeutic agents.
Bibliography:NIH RePORTER
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2010.06.074