抗生素pyrones的两步,高产的总合成
Akram Hussain1, Revoju Sravanthi1,2, Sunitha Katta2
1Catalysis Laboratory, School of Chemistry, University of Hyderabad, Hyderabad-500 046, India. ramsc@uohyd.ac.in.
Organic & biomolecular chemistry
|December 20, 2023
概括
一种新的两步方法从植物性材料中合成了有价值的皮龙抗生素. 这种高效的工艺产生了诸如伪皮龙素和光皮龙素等天然产品,显示出工业潜力.
科学领域:
- 有机化学 有机化学
- 自然产品的合成自然产品的合成
- 药用化学 医学化学
背景情况:
- 皮龙天然产品,包括光皮龙,伪皮龙和紫皮龙,表现出显著的生物活性.
- 对这些复杂分子的获取往往受到具有挑战性的合成路线的限制.
- 生物可再生资源为化学合成提供可持续的原料.
研究的目的:
- 开发一种高效,可扩展的合成协议,用于生物活性的天然产品.
- 为了利用一种易于获得的,生物可再生的原料,三酸乳.
- 为了证明合成的pyrones的功能修饰到各种自然产品的类似物.
主要方法:
- 一个两步的二基化协议被用于最初的合成pyrone支架.
- 随后的O-甲基化反应被用于功能多样化.
- 进行了格拉姆尺度合成,以评估可扩展性和产量.
主要成果:
- 开发的协议在合成光皮龙,伪皮龙和紫皮龙方面取得了很好的产量.
- 四种特定的自然产物 (伪皮龙素A,光皮龙素A,伪皮龙素B和光皮龙素C) 在克拉尺度上进行了合成.
- 该方法在功能性修改成不同的pyrone天然产品方面被证明是有效的.
结论:
- 从三酸乳建立了一个易于和高产的合成途径,以从三酸乳获得重要的激素抗生素.
- 合成策略可以进行工业扩展,为生产这些有价值的化合物提供了可行的途径.
- 这项工作扩大了医学上相关的自然产品的可访问性.
更多相关视频
10:17Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
6.9K
14:11Synthesis of pH Dependent Pyrazole, Imidazole, and Isoindolone Dipyrrinone Fluorophores using a Claisen-Schmidt Condensation Approach
Published on: June 10, 2021
6.2K
相关概念视频
Biosynthesis of Nucleic Acids
Nucleic acid biosynthesis is a fundamental biochemical process that produces the purine and pyrimidine nucleotides essential for DNA and RNA synthesis. This pathway maintains a balanced nucleotide pool, preventing imbalances that could jeopardize genetic integrity and cellular function. Given the crucial role of nucleotides, their synthesis is tightly regulated to ensure proper cellular homeostasis.Purine BiosynthesisThe biosynthesis of purine nucleotides begins with ribose-5-phosphate, a...
Production of Antibiotics
Penicillin, one of the earliest and most widely used antibiotics, is produced industrially by the filamentous fungus Penicillium chrysogenum. Large stirred-tank bioreactors ranging from tens to hundreds of thousands of liters maintain tightly controlled temperature, pH, and dissolved oxygen conditions to support fungal metabolism and maximize antibiotic yield. Penicillin is a secondary metabolite, synthesized primarily during the stationary growth phase, which requires a carefully managed...
Production of Pharmaceuticals
Industrial insulin production uses genetically engineered E. coli expressing a proinsulin gene controlled by a tryptophan promoter and containing a methionine linker for later cleavage. The cells also carry ampicillin resistance for selective growth. Seed cultures are stored at −80 °C and production begins by thawing a small amount to inoculate starter cultures, which are progressively scaled to a 50,000-L bioreactor. In the bioreactor, E. coli grow in nutrient-rich media under sterile, tightly...
