Nielsen Thomas E, Diness Frederik, Meldal Morten
Carlsberg Laboratory, Department of Chemistry, Gamle Carlsberg Vej 10, DK-2500 Valby, Denmark.
Curr Opin Drug Discov Devel. 2003 Nov;6(6):801-14.
The Pictet-Spengler reaction is an important reaction for the generation of tetrahydro-beta-carbolines and tetrahydroisoquinoline ring systems, which exhibit a range of biological and pharmacological properties. This review covers the solid-phase Pictet-Spengler reaction, as employed in solid-phase routes toward a range of complex heterocyclic ring systems, with focus on experimental conditions, efficiency and diastereoselectivity. This is illustrated by the application of this reaction to the synthesis of combinatorial libraries, natural product analogs and drug-like scaffolds.
皮克特-施彭格勒反应是生成四氢-β-咔啉和四氢异喹啉环系的重要反应，这些环系具有一系列生物学和药理学特性。本综述涵盖了用于合成一系列复杂杂环环系的固相皮克特-施彭格勒反应，重点关注实验条件、效率和非对映选择性。通过将该反应应用于组合库、天然产物类似物和类药物支架的合成来说明这一点。
