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通过定向分选法合成一个包含10000个成员的1,5-苯并二氮杂䓬-2-酮文库。

Synthesis of a 10,000 member 1,5-benzodiazepine-2-one library by the directed sorting method.

作者信息

Herpin T F, Van Kirk K G, Salvino J M, Yu S T, Labaudinière R F

机构信息

Rhône-Poulenc Rorer Research and Development, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA.

出版信息

J Comb Chem. 2000 Sep-Oct;2(5):513-21. doi: 10.1021/cc000025u.

DOI:10.1021/cc000025u
PMID:11029177
Abstract

The solid-phase synthesis of a 10,000 member combinatorial library of 1,5-benzodiazepine-2-one derivatives is reported. The 3-amino-1,5-benzodiazepine-2-one scaffold was prepared in solution, and the benzamide nitrogen was used as a point of attachment to the resin. The 5-aniline and 3-amine were then used as points of diversity. A 10,000 member library was synthesized using the Irori directed sorting system, and after analysis of a representative sample from the library, the Irori system was used to remove the compounds of lower purity.

摘要

报道了1,5-苯二氮䓬-2-酮衍生物的10000成员组合库的固相合成。3-氨基-1,5-苯二氮䓬-2-酮支架在溶液中制备,苯甲酰胺氮用作连接到树脂的位点。然后将5-苯胺和3-胺用作多样性位点。使用Irori定向分选系统合成了一个10000成员的库,在对库中的代表性样品进行分析后,使用Irori系统去除纯度较低的化合物。

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