With the flourishing progress of modern medicinal chemistry, bicyclo[1.1.1]pentylamines (BCPAs) have come to the fore as bioisosteres of arylamine motifs to reduce the growing concern about the risks of arylamines related to metabolism, bioavailability, and excretion. In light of the prevalence and significance of BCPAs, an increasing number of new practical protocols to efficiently furnish these appealing molecules have been thus disclosed, which serve to shorten the long synthetic sequences or enable gram-scale syntheses through one-pot multicomponent processes, creating a novel chemical space and systematically streamlining drug design routes.

中文翻译：

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双环[1.1.1]戊胺的合成路线：用于药物设计的蓬勃发展的工具包

随着现代药物化学的蓬勃发展，双环[1.1.1]戊胺（BCPAs）作为芳胺基序的生物等排体脱颖而出，以减少对芳胺与代谢、生物利用度和排泄相关的风险的日益关注。鉴于 BCPA 的普遍性和重要性，因此披露了越来越多的新实用方案来有效地提供这些吸引人的分子，这些方案有助于缩短长合成序列或通过一锅多组分工艺实现克级合成，创造一个新颖的化学空间和系统地简化药物设计路线。