PDF(Pubmed)
Abstract：
The fluorine atom possesses many intrinsic properties that can be beneficial when incorporated into small molecules. These properties include the atom\'s size, electronegativity, and ability to block metabolic oxidation sites. Substituents that feature fluorine and fluorine-containing groups are currently prevalent in drugs that lower cholesterol, relieve asthma, and treat anxiety disorders, as well as improve the chemical properties of various medications and imaging agents. The dye scaffolds (fluorescein/rhodamine, coumarin, BODIPY, carbocyanine, and squaraine dyes) reported will address the incorporation of the fluorine atom in the scaffold and the contribution it provides to its application as an imaging agent. It is also important to recognize radiolabeled fluorine atoms used for PET imaging in the early detection of diseases. This review will discuss the many benefits of incorporating fluorine atoms into small molecules and give examples of fluorinated molecules used in the pharmaceutical industry and imaging techniques.
摘要：
氟原子具有许多固有性质,当掺入到小分子中时,这些性质是有益的。这些属性包括原子的大小，电负性,和阻断代谢氧化位点的能力。以氟和含氟基团为特征的取代基目前在降低胆固醇的药物中普遍存在，缓解哮喘,治疗焦虑症，以及改善各种药物和显像剂的化学性质。染料支架（荧光素/罗丹明，香豆素,BODIPY,碳青,和squaraine染料）报告将解决支架中氟原子的掺入及其对其作为成像剂的应用的贡献。在疾病的早期检测中识别用于PET成像的放射性标记的氟原子也是重要的。这篇综述将讨论将氟原子掺入小分子的许多好处，并给出制药工业和成像技术中使用的氟化分子的例子。
