Properties of Packed Bed Structures Formed during Filtration: A Two and Three-Dimensional Model [0.03%]
过滤过程中形成的固定床结构的特性：二维和三维模型
William Eales,Chris J Price,William Hicks et al.
William Eales et al.
Agglomeration is an issue that causes many problems during secondary processing for pharmaceutical companies, causing material to need further processing and costing additional time and resources to ensure a satisfactory outcome. A potentia...
Quest for a COVID-19 Cure by Repurposing Small-Molecule Drugs: Mechanism of Action, Clinical Development, Synthesis at Scale, and Outlook for Supply [0.03%]
新冠肺炎疫情下小分子药物老药新用的机制、临床开发、规模化合成及供应链展望
Chris De Savi,David L Hughes,Lisbet Kvaerno
Chris De Savi
The outbreak of the COVID-19 pandemic has spurred an intense global effort to repurpose existing approved drugs for its treatment. In this review, we highlight the development of seven small-molecule drugs that are currently being assessed ...
Development of a Large-Scale Cyanation Process Using Continuous Flow Chemistry En Route to the Synthesis of Remdesivir [0.03%]
连续流动化学在瑞德西韦合成路线中大规模氰化工艺的开发
Tiago Vieira,Andrew C Stevens,Andrei Chtchemelinine et al.
Tiago Vieira et al.
The implementation of cyanation chemistry at manufacturing scales using batch equipment can be challenging because of the hazardous nature of the reagents employed and the tight control of reaction parameters, including cryogenic temperatur...
Fei Xue,Xinbo Zhou,Ruijie Zhou et al.
Fei Xue et al.
The bulk supply of the antiviral C-nucleoside analogue remdesivir is largely hampered by a low-yielding C-glycosylation step in which the base is coupled to the pentose unit. Here, we disclose a significantly improved methodology for this c...
Quest for a Cure: Potential Small-Molecule Treatments for COVID-19, Part 2 [0.03%]
寻觅抗疫良药：新冠肺炎潜在小分子药物(下)
David L Hughes
David L Hughes
During the first year of the outbreak of the COVID-19 pandemic, many drugs and drug candidates have been evaluated as treatment options. None yet has proved to be an effective cure, but progress in controlling the disease has been made. In ...
Jule-Philipp Dietz,Dorota Ferenc,Timothy F Jamison et al.
Jule-Philipp Dietz et al.
Di-tert-butyl oxymethyl phosphonates were investigated regarding their suitability for preparing the active pharmaceutical ingredient tenofovir (PMPA). First, an efficient and simple access to the crystalline di-tert-butyl(hydroxymethyl)pho...
Early Clinical Development of Lufotrelvir as a Potential Therapy for COVID-19 [0.03%]
Lufotrelvir用于治疗COVID-19的早期临床开发
Christophe Allais,David Bernhardson,Adam R Brown et al.
Christophe Allais et al.
Lufotrelvir was designed as a first in class 3CL protease inhibitor to treat COVID-19. Development of lufotrelvir was challenged by its relatively poor stability due to its propensity to epimerize and degrade. Key elements of process develo...
Matisyahu S Fogel,Kazunori Koide
Matisyahu S Fogel
Traditionally, new synthetic reactions have been developed using a model substrate to screen reaction conditions before testing the optimized conditions with a range of more complex substrates. In 1998, Gao and Kagan pooled multiple substra...
Toward Kilogram-Scale Peroxygenase-Catalyzed Oxyfunctionalization of Cyclohexane [0.03%]
公斤级过氧化酶催化环己烷氧基官能化反应的研究进展
Thomas Hilberath,Remco van Oosten,Juliet Victoria et al.
Thomas Hilberath et al.
Mol-scale oxyfunctionalization of cyclohexane to cyclohexanol/cyclohexanone (KA-oil) using an unspecific peroxygenase is reported. Using AaeUPO from Agrocybe aegerita and simple H2O2 as an oxidant, cyclohexanol concentrations of more than 3...
Practical and Scalable Two-Step Process for 6-(2-Fluoro-4-nitrophenyl)-2-oxa-6-azaspiro[3.3]heptane: A Key Intermediate of the Potent Antibiotic Drug Candidate TBI-223 [0.03%]
用于潜在抗生素药物候选物TBI-223的关键中间体6-(2-氟-4-硝基苯基)-2-氧杂-6-氮杂螺[3.3]庚烷的实用且可放大的两步制备工艺
Flavio S P Cardoso,Appasaheb L Kadam,Ryan C Nelson et al.
Flavio S P Cardoso et al.
A low-cost, protecting group-free route to 6-(2-fluoro-4-nitrophenyl)-2-oxa-6-azaspiro[3.3]heptane (1), the starting material for the in-development tuberculosis treatment TBI-223, is described. The key bond forming step in this route is th...