
Journal of the American Chemical Society p. 15027 - 15037 (2020)
Update date:2022-08-03
Topics:
McCann, Scott D.
Reichert, Elaine C.
Arrechea, Pedro Luis
Buchwald, Stephen L.
We have developed a new dialkylbiaryl monophosphine ligand, GPhos, that supports a palladium catalyst capable of promoting carbon-nitrogen cross-coupling reactions between a variety of primary amines and aryl halides; in many cases, these reactions can be carried out at room temperature. The reaction development was guided by the idea that the productivity of catalysts employing BrettPhos-like ligands is limited by their lack of stability at room temperature. Specifically, it was hypothesized that primary amine and N-heteroaromatic substrates can displace the phosphine ligand, leading to the formation of catalytically dormant palladium complexes that reactivate only upon heating. This notion was supported by the synthesis and kinetic study of a putative off-cycle Pd complex. Consideration of this off-cycle species, together with the identification of substrate classes that are not effectively coupled at room temperature using previous catalysts, led to the design of a new dialkylbiaryl monophosphine ligand. An Ot-Bu substituent was added ortho to the dialkylphosphino group of the ligand framework to improve the stability of the most active catalyst conformer. To offset the increased size of this substituent, we also removed the para i-Pr group of the non-phosphorus-containing ring, which allowed the catalyst to accommodate binding of even very large α-tertiary primary amine nucleophiles. In comparison to previous catalysts, the GPhos-supported catalyst exhibits better reactivity both under ambient conditions and at elevated temperatures. Its use allows for the coupling of a range of amine nucleophiles, including (1) unhindered, (2) five-membered-ring N-heterocycle-containing, and (3) α-tertiary primary amines, each of which previously required a different catalyst to achieve optimal results.
View MoreFujian Huitian Biological Pharmacy Co., Ltd.
Contact:0086-598-8300831; 8339920
Address:No.46,Taijiang Road,Sanming City,Fujian,China
Contact:18698110882
Address:1303 No2 building,LuoMa Garden,YongAn Road,Hexi District,Tianjin city
Geen Chemical Technology Co., Ltd
Contact:86-769-21660847
Address:1408, Yingfeng Commercial Center, Nancheng District
Shanghai Hanshare Industry Co.,Ltd.
Contact:86 21 20960688
Address:RM902-903,Building E, Wanda Plaza,No.26,Zhoukang Road, Pudong District, Shanghai, China
Almondsea Biological Technology Co., Ltd.
Contact:86-0519-85558333
Address:No 9 Yongsheng Road
Doi:10.1002/ejic.201300334
(2013)Doi:10.1246/bcsj.45.1816
(1972)Doi:10.1021/ol0166597
(2001)Doi:10.1007/s11172-020-2983-4
()Doi:10.1002/anie.201208561
(2013)Doi:10.1002/hlca.19580410636
(1958)