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![Solid-phase Synthesis of [4.4] Spirocyclic Oximes](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F58508.jpg&w=3840&q=50)
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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
这些是Pyrazolopyrimidines
1University of Western Ontario, London Health Sciences Centre, Victoria Campus, 375 South Street, London, Ontario, Canada N6A 4G5. cgeorge@uwo.ca
Lancet (London, England)
|November 22, 2001
概括
针对玛-氨基黄油酸 (GABA) 受体的较新的催眠镇静剂可以改善失眠治疗. 醇胺代表了最新的进步,提供了比旧药物更好的疗效和更少的副作用.
科学领域:
- 药理学 药理学是指药理学的学科.
- 神经科学是一个神经科学.
- 睡眠医学 睡眠医学
背景情况:
- 药物治疗对于治疗失眠至关重要.
- 较老的失眠药物可能会导致耐受性,戒断和白天障碍.
- 对理解胺黄油酸 (GABA) 受体的进步推动了新药的开发.
研究的目的:
- 审查新的催眠镇静剂的开发和有效性.
- 为了比较新型GABA受体选择性剂与较旧的失眠药物的配置.
- 为了强调pyrazolopyrimidines的潜在优势.
主要方法:
- 关于治疗失眠的药理疗法的文献综述.
- 对新催眠药的受体子单元选择性的分析.
- 对疗效和副作用概况的比较评估.
主要成果:
- 新的药物显示了改善的催眠和副作用的特征.
- 对GABA受体子单元的选择性增加导致更好的治疗选择.
- 皮拉佐洛皮里米丁 (Pyrazolopyrimidines) 在现有的催眠药上显示出有前途的优势.
结论:
- 新型GABA受体调节器提供了优越的失眠管理.
- 皮拉佐洛皮里米丁代表了催眠药物治疗的重大进步.
- 这些新药为临床医生和患者提供了增强的治疗选择.
相关概念视频
Five-Membered Heterocyclic Aromatic Compounds: Overview
Heterocyclic aromatic compounds are cyclic compounds that are aromatic and have one or more heteroatoms—atoms other than carbon, in the ring. Depending upon the number of atoms present in the ring, they can be either five or six-membered. Examples of five-membered heterocyclic aromatic compounds include pyrrole, furan, thiophene, and imidazole. Pyrrole consists of one nitrogen atom having one lone pair of electrons. Furan and thiophene have one oxygen and one sulfur heteroatom, respectively.
Basicity of Heterocyclic Aromatic Amines
Heterocyclic amines, where the N atom is a part of an alicyclic system, are similar in basicity to alkylamines. Interestingly, the heterocyclic amine having a nitrogen atom as part of an aromatic ring has much less basicity than its corresponding alicyclic counterpart. For this reason, as presented in Figure 1, piperidine (pKb = 2.8) is significantly more basic than pyridine (pKb = 8.8).
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the para position.
Nomenclature of Aryl and Heterocyclic Amines
The simplest aromatic amine is phenylamine, which contains an –NH2 functionality directly attached to an aromatic ring. The name aniline is designated for this skeleton. As shown in Figure 1, the common names of the functionalized anilines involve prefixes ortho-, meta-, and para- to indicate the substitution position. Different functionalized aniline derivatives also have notable trivial names.
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