Nicholas H McCarthy,Norah S Alsaiari,Thomas Brown et al.
Nicholas H McCarthy et al.
Drying of organic solvates remains hard to scale down and fully understand, as (a) residual solvent is typically hard to remove due to high solid-phase transport resistances, and (b) precise control over crystal properties is challenging. T...
Hectogram-Scale Synthesis of Carbamates Using Electrochemical Hofmann Rearrangement in Flow [0.03%]
流动电流体霍夫曼重排反应克级合成碳酸酯
Darryl F Nater,Rong Zhao,Johannes Rocker et al.
Darryl F Nater et al.
The Hofmann rearrangement of alkyl and aryl carboxamides can be achieved electrochemically on a hectogram scale. The necessary halogen species and base equivalents are generated from sodium bromide in methanol by electrolysis. Both the supp...
Scalable Membrane Enabled One-Pot Liquid-Phase Oligonucleotide Synthesis [0.03%]
可拓展的膜分离 enabled 一步法液相合成寡核苷酸
Ronan Kelly,Catalina Parga,Steven Ferguson
Ronan Kelly
In this article, a new one-pot liquid-phase oligonucleotide synthesis (OP-LPOS) route enabled by organic solvent resistant (OSR) ceramic membranes is described. This approach was demonstrated through the synthesis of 6mer and 18mer 2'-OMe p...
Machine Learning-Driven Optimization of Continuous-Flow Photoredox Amine Synthesis [0.03%]
机器学习驱动的连续流动光氧化还原胺合成优化
Perman Jorayev,Sebastian Soritz,Simon Sung et al.
Perman Jorayev et al.
Photoredox catalysis plays an important role in the synthesis of pharmaceutically relevant compounds such as C-(sp3)-rich tertiary amines. The difficulty of identifying underlying mechanistic models for such novel transformations, coupled w...
Continuous Dihydrolevoglucosenone Recovery Using Commercial Membrane Technology [0.03%]
基于商用膜技术的连续式木质素模型化合物二氢没食子糖酮回收体系
Andreas Dejaegere,Alessandro Napoli,Thomas S A Heugebaert et al.
Andreas Dejaegere et al.
Cyrene, or dihydrolevoglucosenone (DHL), is a biobased and biodegradable solvent that can be produced in two steps from cellulose. It has properties similar to dipolar aprotic solvents such as NMP and DMF, both of which raise significant co...
Surface Defects and Crystal Growth of Apremilast Benzoic Acid Cocrystals [0.03%]
阿普利玛斯特苯甲酸共晶的表面缺陷及晶体生长研究
Jan Jirát,Vít Zvoníček,Luděk Ridvan et al.
Jan Jirát et al.
A cocrystallization process of the active pharmaceutical ingredient apremilast with benzoic acid is explored in this work. The aim of the study is to adjust operating conditions during the crystallization to purposefully tune the dissolutio...
Decagram-Scale Synthesis of the Novel Bacterial Topoisomerase Inhibitor OSUAB-0284 [0.03%]
十亿规模的新型细菌拓扑异构酶抑制剂OSUAB-0284的大规模合成
Jason S West,Chelsea A Mann,Mark J Mitton-Fry
Jason S West
Medicinal chemistry efforts identified OSUAB-0284 (2) as a preclinical candidate to treat staphylococcal infections, especially those caused by methicillin-resistant Staphylococcus aureus (MRSA). Herein, we describe a fit-for-purpose route ...
Development of a Scalable Synthetic Route to (1 R,5 R)-2,2-Dimethoxybicyclo[3.1.0]hexan-3-one: An Important Intermediate in the Synthesis of Lenacapavir [0.03%]
开发通往(1R,5R)-2,2-二甲氧基双环[3.1.0]己烷-3-酮的可扩展合成路线：其为Lenacapavir合成中的重要中间体
Aline Nunes De Souza,Nagaraju Sakkani,Daryl Guthrie et al.
Aline Nunes De Souza et al.
(1R,5R)-2,2-Dimethoxybicyclo[3.1.0]hexan-3-one is used in the asymmetric synthesis of lenacapavir. Herein, we report an enantioselective synthesis of this important chiral intermediate from the inexpensive commodity (R)-epichlorohydrin. Thi...
Impact of Reactant Dissolution in the Kinetics of a Catalytic Hydrogenation for the Production of Argatroban [0.03%]
反应物溶解对催化氢化生产阿加曲班的 kinetics 的影响
Filippo Nanto,Dario Ciato,Mariano Stivanello et al.
Filippo Nanto et al.
An experimental study was performed for a fed-batch catalytic hydrogenation for the production of Argatroban. The penultimate expensive and scarcely available intermediate is characterized by a slow dissolution rate that evolves in parallel...
Scaling Up Gas-Liquid Photo-Oxidations in Flow Using Rotor-Stator Spinning Disc Reactors and a High-Intensity Light Source [0.03%]
使用高强光源和转盘搅拌反应器在流动体系中扩大气液光氧化的规模
Arnab Chaudhuri,Wouter F C de Groot,Jasper H A Schuurmans et al.
Arnab Chaudhuri et al.
Photochemical transformations have garnered renewed interest over the past decade for their ability to enable unique reactions under mild conditions. However, scaling up such processes, particularly in multiphase systems (e.g., gas-liquid),...