Novel solution- and solid-phase strategies for the parallel and combinatorial synthesis of small-molecular-weight compound libraries

被引:0
|
作者
Chucholowski, A [1 ]
Masquelin, T [1 ]
Obrecht, D [1 ]
Stadlwieser, J [1 ]
Villalgordo, JM [1 ]
机构
[1] F HOFFMANN LA ROCHE & CO LTD,PHARMA RES,CH-4070 BASEL,SWITZERLAND
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中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
In this account dedicated to '100 years Roche' in CHIMIA, we present some of our strategies towards the synthesis of interesting novel amino-acid-derived building blocks; multigeneration synthesis of thiazole libraries in solution; a novel solid-phase approach towards highly substituted pyrimidines using a novel safety-catch linker principle and a multidirectional cleavage procedure; a versatile solid-phase synthesis of quinazolones taking advantage of the Staudinger phosphorylimine chemistry combined with a novel cyclization and cleavage strategy, and finally a novel solid-phase diketopiperazine synthesis combining the Ugi four-component reaction with a final ring-forming cleavage step.
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页码:525 / 530
页数:6
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