5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a] diazepine carboxylates are valuable scaffolds for drug design and medicinal chemistry. In this paper we disclose a short scalable synthesis and chemical reactivity patterns of the pyrazolo-diazepine pharmacophore. Commercial and cheaply available Methyl pyrazole 3,5-dicarboxylate was alkylated with 3-bromo-N-Boc propyl amine and the resulting derivative underwent concomitant cyclization upon deprotection of the Boc protecting group to yield the pyrazolo-diazepine skeleton. Selective reduction of the lactam was accomplished cleanly using borane and the resulting amine was pro-tected using a tert-butyloxycarbonyl protecting group. The free N-terminal of the diazepine underwent smooth Buchwald and Chan arylations among various standard chemistry applications examined on this pharmacophore.

中文翻译：

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5,6,7,8-四氢-4H-吡唑并[1,5-a][1,4]二氮杂-2-羧酸酯的合成和化学。

5,6,7,8-四氢-4H-吡唑并[1,5-a]二氮杂羧酸盐是药物设计和药物化学的有价值的支架。在本文中，我们公开了吡唑并二氮杂卓药效团的简短可扩展合成和化学反应模式。将市售且廉价的吡唑3,5-二甲酸甲酯用3-溴-N-Boc丙胺烷基化，所得衍生物在Boc保护基脱保护后进行伴随环化，产生吡唑并二氮杂卓骨架。使用硼烷干净地完成内酰胺的选择性还原，并使用叔丁氧基羰基保护基团保护所得胺。在对该药效团进行检查的各种标准化学应用中，二氮杂卓的游离 N 末端经历了顺利的 Buchwald 和 Chan 芳基化。