Modern organic chemistry is a titan supporting and reinforcing pharmaceutical, agricultural, food and material science products. Over the past decades, the organic compounds market has been evolving to meet all the research demands. In this regard, medicinal chemistry is especially dependent on available chemical space as subtle tuning of the molecule structure is required to create a drug with relevant physicochemical properties and a remarkable activity profile. The recent rapid evolution of synthetic methodology to deploy fluorine has brought fluorinated compounds to the spotlight of MedChem community. And now unique properties of fluorine still keep fascinating more and more as its justified installation into a molecular framework has a beneficial impact on membrane permeability, lipophilicity, metabolic stability, pharmacokinetic properties, conformation, pK_a, etc. The backward influence of medicinal chemistry on organic synthesis has also changed the landscape of the latter towards new fluorinated topologies as well. Such complex relationships create a flexible and ever-changing ecosystem. Given that MedChem investigations strongly lean on the ability to reach suitable building blocks and the existence of reliable synthetic methods in this review we collected advances in the chemistry of respectful, but still enigmatic gem-difluorinated aza-heterocyclic building blocks.

中文翻译：

---

具有环内 CF2 片段的氮杂杂环砌块

现代有机化学是医药、农业、食品和材料科学产品的强大支持和强化。在过去的几十年里，有机化合物市场一直在不断发展，以满足所有的研究需求。在这方面，药物化学尤其依赖于可用的化学空间，因为需要对分子结构进行微妙的调整来创造具有相关物理化学性质和显着活性特征的药物。最近，氟合成方法的快速发展使氟化化合物成为 MedChem 界关注的焦点。如今，氟的独特性质仍然越来越令人着迷，因为它被合理地安装到分子框架中，对膜的通透性、亲脂性、代谢稳定性、药代动力学性质、构象、pKa等产生有益的影响。_药物化学的落后影响对有机合成的研究也改变了后者的面貌，转向新的氟化拓扑。这种复杂的关系创造了一个灵活且不断变化的生态系统。鉴于 MedChem 的研究强烈依赖于获得合适结构单元的能力以及可靠合成方法的存在，在本次综述中，我们收集了令人尊敬但仍然神秘的宝石二氟化氮杂环结构单元的化学进展。