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Aminocarbonylation of Aryl Tosylates to Carboxamides
被引:18
|作者:
Chung, Seungwon
[1
]
Sach, Neal
[3
]
Choi, Chulho
[1
]
Yang, Xiaojing
[1
]
Drozda, Susan E.
[1
]
Singer, Robert A.
[2
]
Wright, Stephen W.
[1
]
机构:
[1] Pfizer Global Res & Dev, Biotherapeut Chem, Groton, CT 06340 USA
[2] Pfizer Global Res & Dev, Chem Res & Dev, Groton, CT 06340 USA
[3] Pfizer Global Res & Dev, Oncol Chem, La Jolla, CA 92121 USA
关键词:
PALLADIUM-CATALYZED CARBONYLATION;
CROSS-COUPLING REACTIONS;
ARYLBORONIC ACIDS;
MESYLATES;
HALIDES;
ALKOXY;
ALKOXYCARBONYLATION;
ARENESULFONATES;
CHLORIDES;
PHENOLS;
D O I:
10.1021/acs.orglett.5b01283
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
The palladium - catalyzed aminocarbonylation of aryl tosylates with amines is reported. Suitable conditions were identified by high throughput reaction screening and then further optimized. The substrate scope of the reaction with respect to the aryl tosylate component and the amine component are reported. Competitive aminolysis of the aryl tosylates to afford the amine toluenesulfonamides and the phenol was not observed.
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页码:2848 / 2851
页数:4
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