Employing Constant Rate Filtration To Assess Active Pharmaceutical Ingredient Washing Efficiency [0.03%]
采用恒定速率过滤法评估药物活性成分洗涤效率
Muhid Shahid,Chloé Faure,Sara Ottoboni et al.
Muhid Shahid et al.
Washing is a key step in pharmaceutical isolation to remove unwanted crystallization solvents and dissolved impurities (mother liquor) from the active pharmaceutical ingredient (API) filter cake to ensure the purity of the product whilst ma...
Facile and Scalable Methodology for the Pyrrolo[2,1- f][1,2,4]triazine of Remdesivir [0.03%]
用于瑞德西韦合成的苯并三氮唑类药物的简便可放大量合成方法论研究
Sarabindu Roy,Ajay Yadaw,Subho Roy et al.
Sarabindu Roy et al.
Pyrrolo[2,1-f][1,2,4]triazine (1) is an important regulatory starting material in the production of the antiviral drug remdesivir. Compound 1 was produced through a newly developed synthetic methodology utilizing simple building blocks such...
Development of a Robust Manufacturing Route for Molnupiravir, an Antiviral for the Treatment of COVID-19 [0.03%]
一种用于治疗新冠肺炎的抗病毒药物莫纳皮拉韦(Molnupiravir)的稳健制造工艺开发
Patrick S Fier,Yingju Xu,Marc Poirier et al.
Patrick S Fier et al.
Herein is described the development of a large-scale manufacturing process for molnupiravir, an orally dosed antiviral that was recently demonstrated to be efficacious for the treatment of patients with COVID-19. The yield, robustness, and ...
Generation of Tosyl Azide in Continuous Flow Using an Azide Resin, and Telescoping with Diazo Transfer and Rhodium Acetate-Catalyzed O-H Insertion [0.03%]
基于偶氮树脂连续流生成对甲苯磺酰基叠氮化物及其与偶氮转移和醋酸铑催化O-H插入串联反应
Rosella M O&#x;Mahony,Denis Lynch,Katie S O&#x;Callaghan et al.
Rosella M O&#x;Mahony et al.
Generation of tosyl azide 12 in acetonitrile in flow under water-free conditions using an azide resin and its use in diazo transfer to a series of aryl acetates are described. Successful telescoping with a rhodium acetate-catalyzed O-H inse...
Toward a Practical, Nonenzymatic Process for Investigational COVID-19 Antiviral Molnupiravir from Cytidine: Supply-Centered Synthesis [0.03%]
以胞苷为原料的 investigational COVID-19 抗病毒药物 Molnupiravir 的非酶生产研究及合成供给路径探索
Vijayagopal Gopalsamuthiram,Appasaheb L Kadam,Jeffrey K Noble et al.
Vijayagopal Gopalsamuthiram et al.
A scalable four-step synthesis of molnupiravir from cytidine is described herein. The attractiveness of this approach is its fully chemical nature involving inexpensive reagents and more environmentally friendly solvents such as water, isop...
Deracemization via Periodic and Non-periodic Temperature Cycles: Rationalization and Experimental Validation of a Simplified Process Design Approach [0.03%]
通过周期和非周期温度循环进行消旋：简化过程设计方法的合理化及实验验证
Francesca Breveglieri,Brigitta Bodák,Marco Mazzotti
Francesca Breveglieri
Solid-state deracemization via temperature cycles is a promising technique that combines crystallization and racemization in the same batch process to attain enantiomer purification. This method is particularly attractive because the target...
Preparative Synthesis of an R P-Guanosine-3',5'-Cyclic Phosphorothioate Analogue, a Drug Candidate for the Treatment of Retinal Degenerations [0.03%]
R-P鸟苷-3',5'-环磷硫代酸酯类似物的半制备性合成，一种用于治疗视网膜变性的候选药物
Oswaldo Pérez,Nicolaas Schipper,Martin Bollmark
Oswaldo Pérez
Cyclic guanosine monophosphorothioate analogue 1a is currently showing potential as a drug for the treatment of inherited retinal neurodegenerations. To support ongoing preclinical and clinical work, we have developed a diastereoselective s...
Defining the Qualities of High-Quality Palladium on Carbon Catalysts for Hydrogenolysis [0.03%]
氢解反应载钯碳催化剂高活性及长寿命的定义属性研究
Conor J Crawford,Yan Qiao,Yequn Liu et al.
Conor J Crawford et al.
Palladium-catalyzed hydrogenolysis is often the final step in challenging natural product total syntheses and a key step in industrial processes producing fine chemicals. Here, we demonstrate that there is wide variability in the efficiency...
A Novel Integrated Workflow for Isolation Solvent Selection Using Prediction and Modeling [0.03%]
基于预测和建模的新型综合工作流程用于隔离溶剂选择
Sara Ottoboni,Bruce Wareham,Antony Vassileiou et al.
Sara Ottoboni et al.
A predictive tool was developed to aid process design and to rationally select optimal solvents for isolation of active pharmaceutical ingredients. The objective was to minimize the experimental work required to design a purification proces...
Computer Aided Design of Solvent Blends for Hybrid Cooling and Antisolvent Crystallization of Active Pharmaceutical Ingredients [0.03%]
用于活性药物成分混合冷却和非溶剂结晶的溶剂混配计算机辅助设计
Oliver L Watson,Suela Jonuzaj,John McGinty et al.
Oliver L Watson et al.
Choosing a solvent and an antisolvent for a new crystallization process is challenging due to the sheer number of possible solvent mixtures and the impact of solvent composition and crystallization temperature on process performance. To fac...