US 7,375,234 B2
Copper-catalysed ligation of azides and acetylenes
K. Barry Sharpless, La Jolla, Calif. (US); Valery Fokin, Oceanside, Calif. (US); Vsevold A. Rostovtsev, Wilmington (Germany); Luke Green, Basel (Switzerland); and Fahmi Himo, Solna (Sweden)
Assigned to The Scripps Research Institute, La Jolla, Calif. (US)
Appl. No. 10/516,671
PCT Filed May 30, 2003, PCT No. PCT/US03/17311
§ 371(c)(1), (2), (4) Date May 16, 2005,
PCT Pub. No. WO03/101972, PCT Pub. Date Dec. 11, 2003.
Claims priority of provisional application 60/385041, filed on May 30, 2002.
Prior Publication US 2005/0222427 A1, Oct. 06, 2005
Int. Cl. C07D 249/04 (2006.01); C07D 249/06 (2006.01); C07D 403/06 (2006.01); C07D 403/14 (2006.01)
U.S. Cl. 548—255 6 Claims
 
1. A Cu(I) catalyzed process for preparing a 1,4-disubstituted 1,2,3-triazole comprising:
contacting an organic azide and a terminal alkyne with a catalytic quantity of Cu(I) ion for a time sufficient to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole.