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一个用于合成化叶酸衍生物的通用协议

Jie Li¹, Yao Wang¹, Liangang Shan¹

¹Institute of Hybrid Materials, National Center of International Research for Hybrid Materials Technology, National Base of International Science & Technology Cooperation, College of Materials Science and Engineering, Qingdao University, Qingdao 266071, China.

Molecules (Basel, Switzerland)

|July 14, 2023

概括

一种新的,具有成本效益的方法合成了化叶酸 (TFa) 用于药物输送. 这种多功能TFa很容易附着在纳米颗粒上,增强向治疗和诊断.

科学领域:

生物结合化学生物结合化学
纳米医学是一种纳米医学.
药物输送系统药物输送系统

背景情况:

叶酸 (FA) 对于向药物输送和诊断非常有价值,因为它具有向瘤的能力,生物相容性和可负担性.
目前将FA纳入药物输送系统的方法涉及复杂的合成,导致产量低,成本高.

研究的目的:

开发一种通用,高效的协议,用于合成小分子二氧化叶酸 (TFa) 衍生物.
为了证明TFa在修改纳米颗粒的潜在生物应用中的实用性.

主要方法:

一个新的绿色氧化协议在没有催化剂的情况下在水中合成了含有S-S的二醇.
叶酸与二醇进行了化,随后进行了二硫化键裂解,以获得TFa (>98.20%纯度).
合成的TFa被用来使银纳米粒子功能化.

主要成果:

绿色氧化方案产生了纯度>99.44%的二醇.
开发的协议有效地合成了TFa,一种小分子二氧化叶酸衍生物.
TFa表现出易于与金属纳米颗粒结合,表明其对纳米医学应用的潜力.

结论:

建立了一个用于合成硫化叶酸衍生物的通用和有效的协议.
合成的TFa适用于轻松修改纳米粒子.
这种方法提供了一种具有成本效益和多功能性的方法,以增强叶酸在向治疗和诊断中的生物应用.

关键词:

叶酸是叶酸的一种.银纳米颗粒的使用方法硫酸硫酸的使用方法有针对性的交付目标.硫化叶酸硫化叶酸是什么意思

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相关概念视频

Preparation and Reactions of Thiols

Preparation and Reactions of Thiols

Thiols are prepared using the hydrosulfide anion as a nucleophile in a nucleophilic substitution reaction with alkyl halides. For instance, bromobutane reacts with sodium hydrosulfide to give butanethiol.

Preparation and Reactions of Sulfides

Preparation and Reactions of Sulfides

Sulfides are the sulfur analog of ethers, just as thiols are the sulfur analog of alcohol. Like ethers, sulfides also consist of two hydrocarbon groups bonded to the central sulfur atom. Depending upon the type of groups present, sulfides can be symmetrical or asymmetrical. Symmetrical sulfides can be prepared via an SN2 reaction between 2 equivalents of an alkyl halide and one equivalent of sodium sulfide.