A one-pot process for the microwave-assisted synthesis of 7-substituted pyrazolo[1,5-a] pyrimidine

被引:16
|
作者
Bassoude, Ibtissam [1 ,2 ]
Tber, Zahira [1 ]
Essassi, El Mokhtar [2 ,3 ]
Guillaumet, Gerald [1 ]
Berteina-Raboin, Sabine [1 ]
机构
[1] Univ Orleans, Inst Chim Organ & Analyt, UMR CNRS 7311, F-45067 Orleans, France
[2] Univ Mohammed V Agdal, Fac Sci, Lab Chim Organ Heterocycl URAC 21, Rabat 10100, Morocco
[3] RABAT Design Ctr, Ctr Composites & Nanocomposites, MAScIR, Rabat 10100, Morocco
关键词
CATALYZED ALPHA-ARYLATION; ESTROGEN-RECEPTOR LIGANDS; CARBONYL-COMPOUNDS; PALLADIUM; DISCOVERY; OPTIMIZATION; ANTAGONISTS; ACETAMIDES; INHIBITORS; KETONES;
D O I
10.1039/c5ra23417d
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
An efficient synthesis of 7-substituted pyrazolo[1,5-a] pyrimidines using a one-pot, two-step process via Pd-catalyzed direct CH-arylation followed by a saponification-decarboxylation reaction is reported. Compared to the classical method (Negishi coupling), this new procedure has the advantages of convenient manipulation, short reaction times, excellent yields and the use of commercially available and relatively non-toxic compounds.
引用
收藏
页码:3301 / 3306
页数:6
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