作者:Henrik C. Hansen、Roger Olsson、Glenn Croston、Carl-Magnus Andersson
DOI:10.1016/s0960-894x(00)00483-2
日期:2000.11
A flexible, multistep parallel synthesis of spiperone analogues is described. A library of 4-substituted piperidines, assembled utilizing reductive amination and acylation protocols, was alkylated either homogeneously or heterogeneously, exploiting a product release only concept, to afford an oxa-series of spiperone analogues. Screening of the products at 5-HT2 and D2 receptors revealed 5-HT2A antagonists
描述了蝶啶类似物的灵活的多步平行合成。利用还原胺化和酰化方案组装的4-取代的哌啶文库利用仅产品释放的概念被均一或异质地烷基化,以提供oxa系列的spiperone类似物。对5-HT2和D2受体产物的筛选显示,与烯酮和AMI-193相比,选择性更高的5-HT2A拮抗剂。