Dendrimer-supported combinatorial chemistry

被引:83
作者
Kim, RM
Manna, M
Hutchins, SM
Griffin, PR
Yates, NA
Bernick, AM
Chapman, KT
机构
[1] Dept. of Molec. Design and Diversity, Merck Research Laboratories, Rahway
关键词
combinatorial chemistry; dendrimer; size exclusion chromatography; solution phase synthesis;
D O I
10.1073/pnas.93.19.10012
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
A new methodology for the construction of combinatorial libraries is described. The approach, termed dendrimer-supported combinatorial chemistry (DCC), centers on the use of dendrimers as soluble supports, Salient features of DCC include solution phase chemistry, homogeneous purification, routine characterization of intermediates, and high support loadings. To demonstrate the feasibility of DCC, single compounds and a small combinatorial library were prepared via the Fischer indole synthesis. Excellent product yields and purities were obtained, and dendrimer-protected intermediates could be routinely analyzed by H-1 and C-13 NMR and by mass spectrometry. The results indicate that DCC is a general and efficient strategy for the generation of combinatorial libraries.
引用
收藏
页码:10012 / 10017
页数:6
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