A general and efficient Cu(I)-mediated cross-coupling and heterocyclization reaction of 3-iodoimidazo[1,2-a]pyridine-2-carboxylic acid, and terminal alkynes was developed under very mild conditions. This method allows the introduction in one pot of a third ring fused in positions 2 and 3 of the imidazo[1,2-a]pyridine core with reasonable yields and total regioselectivity. This procedure does not require the use of any expensive supplementary additives, and is palladium-free.

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C h emIn fo rm 2 0 1 2 , 4 3 , issu e 1 0 © 2 0 1 2 Wiley -VCH Verl ag G m b H & Co. K G a A , We i n he i m Sulfonam ides Q 0 560 DOI: 1 0.100 2/ch in.201 2100 73 E fficient Preparatio n of ortho -Aminobenzen esulf o namides Us ing L ig and-F ree Coppe r(I) -Catalyz ed Amination. -A sim ple me thod is pr es ented for the pre para tion o f p h arm a ce u tica lly im p o rtan t title co m po u n ds (III) . -(BA HL AO UA N, Z.; TH I BO NN E T , J . ; D UC HE N E, A. ; PA RR AI N , J . -L. ; E L HI L AL I , M. ; AB AR BR I *, M. ; Synle tt 201 1, 17, 2509 -2 512, http://dx .doi.org /10.10 55/s-0030-1 26032 3 ; Lab . Phys.-C h im. Mate riaux B iom ol., Fa c. Sc i., Univ. Fr a nc ois-Rab elais, F-37 200 To urs, Fr.; Eng.) -Ma is 10 -07 3

Copper(I)-Mediated Preparation of New Pyrano[3',4':4,5]imidazo[1,2-a]pyridin--1-one Compounds underMild Palladium-Free Conditions. -The methodology does not involve the use of an expensive, air-sensitive palladium(0) catalyst or any additive ligand. -(BAHLAOUAN, Z.; ABARBRI*, M.; DUCHENE, A.; THIBONNET, J.; HENRY, N.; ENGUEHARD-GUEIFFIER, C.; GUEIFFIER, A.; Org. Biomol. Chem. 9 (2011) 4, 1212-1218, http://dx.doi.org/10.1039/c0ob00622j ; Lab. Phys.-Chim. Materiaux Biomol., Fac. Sci., Univ. Francois-Rabelais, F-37200 Tours, Fr.; Eng.) -Bartels 25-160

A general and efficient method of copper-catalyzed amination of 2-iodobenzenesulfonamide has been developed under very mild conditions, with good to excellent yields. This method uses inexpensive copper(I) iodide as catalyst, readily available 2-iodobenzenesulfonamides and aliphatic amines as the starting materials, and does not require the use of any ligand system or any expensive supplementary additives.