What can we say?

CPhI is really important and we had some very important activities going on, such as preparing the official GalChimiApplus presentation. However, the work for the newsletter was done, so here is the selection for October.

Highly Practical Copper(I)/TEMPO Catalyst System for Chemoselective Aerobic Oxidation of Primary Alcohols

Looks like a quick, clean oxidation of primary alcohols.

J. Am. Chem. Soc., 2011, 133 (42), pp 16901–16910. See: 10.1021/ja206230h

Copper-Mediated C–H Activation/C–S Cross-Coupling of Heterocycles with Thiols

C-H activation of benzothiazoles and introduction of thiols in the C-2.

J. Org. Chem., 2011, 76 (21), pp 8999–9007. See: 10.1021/jo2017444

Palladium-Catalyzed Hiyama Cross-Coupling of Aryltrifluorosilanes with Aryl and Heteroaryl Chlorides

Hiyama coupling using aryltrifluorosilanes (exotic) and chlorides as partners.

J. Org. Chem., 2011, 76 (21), pp 9182–9187. See: 10.1021/jo201840n

NiCl2(PMe3)2-Catalyzed Borylation of Aryl Chlorides

An alternative to the usual borylation with Palladium, and you can use also chlorides.

Org. Lett., 2011, 13 (21), pp 5766–5769. See: 10.1021/ol202267t

Synthesis of Pyrazoles via CuI-Mediated Electrophilic Cyclizations of a,b-Alkynic Hydrazones

Anything giving pyrazoles regioselectively is worthwile.

J. Org. Chem., 2011, 76 (22), pp 9379–9390. See: 10.1021/jo201685p

Silver-Mediated Trifluoromethylation of Arenes Using TMSCF3

As we said in other part of this issue, we will open a new section under this headline.

Org. Lett., 2011, 13 (20), pp 5464–5467. See: 10.1021/ol202174a

Copper-Mediated Cyanation of Aryl Halide with the Combined Cyanide Source

Quite similar to another paper we selected for issue 19, but in this case using Cu instead Pd.

Org. Lett., 2011, 13 (19), pp 5004–5007. See: 10.1021/ol201713b

One-Pot Two-Component [3 + 2] Cycloaddition/Annulation Protocol for the Synthesis of Highly Functionalized Thiophene Derivatives

You can prepare trisubstituted thiophenes in a one pot reaction. That’s worthwile for any med chem proud of that name.

Palladium-Catalyzed Direct Arylation of Heteroaromatic Compounds: Improved Conditions Utilizing Controlled Microwave Heating

A microwave synthesis paper by Kappe. I can’t say no, honestly.

J. Org. Chem., 2011, 76 (19), pp 8138–8142. See: 10.1021/jo201516v