Treatment of 3-bromopyrazolo[1,5-a]pyrimidine with a variety of 1° or 2° alkylamines with 20 mol% CuI, 40 mol% l-proline, and Et₃N (2 equiv) in DMSO under microwave heating at 130 °C (4 h) gave the corresponding C-3 aminated products in good to excellent isolated yields (54–90 %; ave. yield = 77 %). The reaction worked well for simple 1° alkylamines (e.g. butylamine, benzylamine, cyclohexylamine, and isopropylamine), and 1° amines with CH₂- or CH₂CH₂-linked heterocycles (e.g. furan, thiophene, pyridine, and/or indole) were also well tolerated. 2° Alkylamines were also good substrates for this reaction (e.g. piperidine, pyrrolidine, and morpholine). The reaction worked well under conventional heating conditions on both the mg or gram-scales, with representative gram-scale reactions giving products in 72–76 % yield under conventional heating. Coupling to a pegylated azide (11-azido-3,6,9-trioxaundecan-1-amine, 65 % yield microwave) demonstrated compatibility of this coupling methodology for potential click-type conjugation of the pyrazolo[1,5-a]pyrimidine to biologically relevant target ligands.

3-溴吡唑并 [1,5- a ] 嘧啶与各种 1° 或 2° 烷基胺与 20 mol% CuI、40 mol% l-脯氨酸和 Et ₃ N（2 当量）在 DMSO 中微波加热下处理130 °C（4 小时）得到相应的 C-3 胺化产物，分离产率良好至极佳（54–90%；平均产率 = 77%）。该反应适用于简单的 1° 烷基胺（例如丁胺、苄胺、环己胺和异丙胺）和带有 CH ₂ - 或 CH ₂ CH _{2的 1° 胺}-连接的杂环化合物（例如呋喃、噻吩、吡啶和/或吲哚）也具有良好的耐受性。2°烷基胺也是该反应的良好底物（例如哌啶、吡咯烷和吗啉）。该反应在常规加热条件下在 mg 或克尺度上都表现良好，具有代表性的克尺度反应在常规加热下以 72-76% 的产率生成产物。与聚乙二醇化叠氮化物（11-叠氮基-3,6,9-三氧杂环十二烷-1-胺，65% 产率微波）的偶联证明了这种偶联方法与吡唑并 [1,5-a] 嘧啶的潜在点击型共轭的相容性生物学相关的靶配体。