Rapid and Efficient Pd-Catalyzed Sonogashira Coupling of Aryl

Rapid and Efficient Pd-Catalyzed Sonogashira Coupling of Aryl Chlorides

TABLE 1.

Optimization of Catalysis Conditionsa

He Huang, Hong Liu,* Hualiang Jiang, and Kaixian Chen Drug DiscoVery and Design Centre, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, and Graduate School, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China [email protected] ReceiVed May 11, 2008

entry

solvent

palladium

phosphane

1 2 3 4 5 6 7 8 9

DMSO DMSO DMSO DMSO DMSO DMSO DMSO DMSO DMF

PdCl2(PPh3)2 PdCl2(PPh3)2 PdCl2(PPh3)2 PdCl2 Pd(OAc)2 PdCl2(PPh3)2 PdCl2(PPh3)2 PdCl2(PPh3)2 PdCl2(PPh3)2

PPh3 PtBu3 PtBu3 PtBu3 PtBu3 PtBu3 PtBu3 PtBu3

base

yield [%]

Cs2CO3 NaOMe NaOEt Cs2CO3

0