A short and efficient synthesis of 3-{2-[2-(bromomethyl)thiazol-4-yl]- ethynyl}-5-fluorobenzonitrile: A precursor for PET radioligand [ 18F]SP203

Synthesis

Volumn , Issue 12, 2009, Pages 1979-1982

  Gopinathan, Madathil B ^a   Jin, Chunyang ^a   Rehder, Kenneth S ^a  

^a RTI INTERNATIONAL   (United States)

Author keywords

Bromination; Fluorine; Palladium; PET ligand; Sonogashira coupling

Indexed keywords

BROMINATION; EFFICIENT SYNTHESIS; ETHYNYL; PET LIGAND; PET RADIOLIGAND; SONOGASHIRA COUPLING; SYNTHON; TITLE COMPOUNDS;

FLUORINE; LIGANDS; PALLADIUM;

CHEMICAL REACTIONS;

3 [2 [2 (BROMOMETHYL)THIAZOL 4 YL]ETHYNYL] 5 FLUOROBENZONITRILE; 3 FLUORO 5 [2 [2 (FLUOROMETHYL)THIAZOL 4 YL]ETHYNYL]BENZONITRILE F 18; RADIOLIGAND; RADIOPHARMACEUTICAL AGENT; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; BROMINATION; DRUG SYNTHESIS; POSITRON EMISSION TOMOGRAPHY; SONOGASHIRA REACTION;

EID: 67650076588     PISSN: 00397881     EISSN: 1437210X     Source Type: Journal    
DOI: 10.1055/s-0029-1216787     Document Type: Article

References (8)

1. Ozawa, S.; Kamiya, H.; Tsuzuki, K. Prog. Neurobiol. 1998, 54, 581.
2. Conn, P. J.; Pin, J.-P. Ann. Rev. Pharmacol. Toxicol. 1997, 37, 205.
3. Pin, J. P.; Acher, F. Curr. Drug Targets: CNS Neurol. Disord. 2002, 1, 297.
4. Cosford, N. D. P.; Roppe, J.; Tehrani, L.; Schweiger, E. J.; Seiders, T. J.; Chaudary, A.; Rao, S.; Varney, M. A. Bioorg. Med. Chem. Lett. 2003, 13, 351.
5. Alagille, D.; Baldwin, R. M.; Roth, B. L.; Wroblewski, J. T.; Grajkowska, E.; Tamagman, G. D. Bioorg. Med. Chem. 2005, 13, 197.
6. Siméon, F. G.; Brown, A. K.; Zoghbi, S. S.; Patterson, V. M.; Innis, R. B.; Pike, V. W. J. Med. Chem. 2007, 50, 3256.
7. Shetty, H. U.; Zoghbi, S. S.; Siméon, F. G.; Liow, J. S.; Brown, A. K.; Kannan, P.; Innis, R. B.; Pike, V. W. J. Pharmacol. Exp. Ther. 2008, 327, 727.
8. Brown, A. K.; Kimura, Y.; Zoghbi, S. S.; Siméon, F. G.; Liow, J.-S.; Kreisl, W. C.; Taku, A.; Fujita, M.; Pike, V. W.; Innis, R. B. J. Nucl. Med. 2008, 49, 2042.