生成 500 成员的 10-烷基-2-R(1),3-R(2)-4,10-二氢苯并[4,5]咪唑[1,2-α]嘧啶-4-酮文库。

Department of Chemistry of Heterocyclic Compounds, SSI Institute for Single Crystals of National Academy of Sciences of Ukraine, Lenin Ave. 60, Kharkiv 61001, Ukraine.

Molecules. 2009 Dec 15;14(12):5223-34. doi: 10.3390/molecules14125223.

Representative benzimidazopyrimidinones were previously reported to be intercalating antitumor agents. In this work, we used 2-substituted 4,10-dihydrobenzo [4,5]imidazo[1,2-alpha]pyrimidin-4-ones for their diversification by regioselective alkylation. Under the conditions established, the alkylation gave 10-alkyl derivatives which permitted the parallel generation of a 500-member library of the title compounds.

先前有报道称，代表性苯并咪唑并嘧啶酮是嵌入型抗肿瘤剂。在这项工作中，我们使用 2-取代的 4,10-二氢苯并[4,5]咪唑并[1,2-α]嘧啶-4-酮，通过区域选择性烷基化对其进行多样化处理。在建立的条件下，烷基化得到了 10-烷基衍生物，这允许平行生成 500 个标题化合物的文库。