Rapid Assessment of Protecting- Group Stability by Using a Robustness Screen

被引:29
作者
Collins, Karl D. [1 ]
Ruehling, Andreas [1 ]
Lied, Fabian [1 ]
Glorius, Frank [1 ]
机构
[1] Univ Munster, Inst Organ Chem, D-48149 Munster, Germany
关键词
arylation; heterocycles; high-throughput screening; protecting groups; robustness screen; H BOND ARYLATION; ARYLBORONIC ACIDS; THIOPHENES; ACTIVATION; PYRAZOLES; CATALYST; COUPLINGS; ACCESS; SYSTEM; SALTS;
D O I
10.1002/chem.201304508
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
An experimentally simple method has been developed to rapidly establish the stability of widely utilized silyl, acetal, and carbamate protecting groups to a given set of reaction conditions. Assessment of up to twelve protecting groups in a single experiment has been demonstrated. Evaluation of this protocol in two unrelated synthetic transformations suggests that this method can be used to select appropriate protecting groups in the design of synthetic routes.
引用
收藏
页码:3800 / 3805
页数:6
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