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相关概念视频

Preparation of Amides01:29

Preparation of Amides

3.0K
Amides are synthesized by treating carboxylic acids with amines in the presence of dehydrating agents like dicyclohexylcarbodiimide (DCC).
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
3.0K
E2 Reaction: Kinetics and Mechanism02:45

E2 Reaction: Kinetics and Mechanism

10.3K
SN2 substitutions and E2 eliminations of alkyl halides proceed via a concerted pathway. While the nucleophile attacks the alpha carbon in SN2 reactions, it functions as a strong base and abstracts a beta hydrogen in the E2 mechanism. The rate-limiting transition state in E2 elimination reactions is characterized by partially broken carbon–hydrogen and carbon–halogen bonds and a partially formed pi bond between the alpha and beta carbons. The beta hydrogen and halide are eliminated...
10.3K
Aldol Condensation with β-Diesters: Knoevenagel Condensation01:27

Aldol Condensation with β-Diesters: Knoevenagel Condensation

3.0K
The Knoevenagel condensation is an aldol-type reaction involving the condensation of aldehydes or ketones with active methylene compounds such as β-diesters to produce substituted olefins.
3.0K
Acid-Catalyzed Ring-Opening of Epoxides02:24

Acid-Catalyzed Ring-Opening of Epoxides

7.3K
Epoxides that are three-membered ring systems are more reactive than other cyclic and acyclic ethers. The high reactivity of epoxides originates from the strain present in the ring. This ring strain acts as a driving force for epoxides to undergo ring-opening reactions either with halogen acids or weak nucleophiles in the presence of mild acid. The acid catalyst converts the epoxide oxygen, a poor leaving group, into an oxonium ion, a better leaving group, making the reaction feasible. The...
7.3K
Amines to Amides: Acylation of Amines01:19

Amines to Amides: Acylation of Amines

2.5K
Various carboxylic acid derivatives (such as acid chlorides, esters, and anhydrides) can be used for the acylation of amines to yield amides. The reaction requires two equivalents of amines. The first amine molecule functions as a nucleophile and attacks the carbonyl carbon to produce a tetrahedral intermediate. This is followed by the loss of the leaving group and restoration of the C=O bond.
Next, the second equivalent of amine serves as a Brønsted base and deprotonates the quaternary...
2.5K
Alkylation of β-Ketoester Enolates: Acetoacetic Ester Synthesis01:07

Alkylation of β-Ketoester Enolates: Acetoacetic Ester Synthesis

3.3K
Acetoacetic ester synthesis is a method to obtain ketones from alkyl halides and β-keto esters. The reaction occurs in the presence of an alkoxide base that abstracts the acidic proton of the β-keto esters. The step results in an enolate ion which is doubly stabilized. The enolate then reacts with an alkyl halide via the SN2 process to produce an alkylated ester intermediate with a new C–C bond. The hydrolysis of the intermediate, followed by acidification, results in an...
3.3K

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Synthesis of Esters Via a Greener Steglich Esterification in Acetonitrile
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用于EDC介导的胺合成的反应性深度环氧溶剂.

Debora Procopio1, Carlo Siciliano1, Maria Luisa Di Gioia1

  • 1Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036, Arcavacata of Rende, Italy. ml.digioia@unical.it.

Organic & biomolecular chemistry
|December 21, 2023
PubMed
概括

这项研究介绍了一种使用反应性深层阳性溶剂 (RDESs) 的更绿色的胺合成方法. 这种可持续的方法避免了危险的溶剂,并简化了净化,推进了环保的制药生产.

科学领域:

  • 绿色化学是一种绿色化学.
  • 有机合成 有机合成
  • 制药制造业 制药制造业 制药制造业

背景情况:

  • 氨基酸键的形成在药品中至关重要,但传统方法往往缺乏可持续性.
  • 开发环保的胺合成仍然是行业面临的重大挑战.

研究的目的:

  • 开发一种更绿色,更有效的胺合成方法.
  • 为了利用反应性深性溶剂 (RDESs) 作为反应介质和反应剂.

主要方法:

  • 采用RDES用于胺基键形成,消除危险的溶剂.
  • 实施一种简单的产品回收程序,而不需要染色学净化.
  • 应用该方法来合成阿提诺洛尔的关键中间体.

主要成果:

  • 该RDES方法在胺合成中显示出高纯度和高效率.
  • 取得了有效药物成分中间体的成功合成.
  • 格拉姆尺度比较显示,绿色指标比传统策略有所改善.

结论:

  • 反应性深层阳性溶剂为胺合成提供了可持续和高效的替代方案.
  • 这种方法代表了绿化制药制造工艺的重大进展.

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