A5008513311- Biochemical and Molecular Research
- Chemical Synthesis and Analysis
- HIV/AIDS drug development and treatment
- Cancer therapeutics and mechanisms
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Forensic Toxicology and Drug Analysis
- Psychedelics and Drug Studies
- Microwave-Assisted Synthesis and Applications
- Cannabis and Cannabinoid Research
- Asymmetric Hydrogenation and Catalysis
- Quinazolinone synthesis and applications
- Synthesis and Biological Evaluation
- Oxidative Organic Chemistry Reactions
- Microbial Natural Products and Biosynthesis
- Inflammatory mediators and NSAID effects
- Click Chemistry and Applications
- Synthetic Organic Chemistry Methods
- Innovative Microfluidic and Catalytic Techniques Innovation
- Multicomponent Synthesis of Heterocycles
- Fluorine in Organic Chemistry
- Tuberculosis Research and Epidemiology
- Sulfur-Based Synthesis Techniques
- Neurotransmitter Receptor Influence on Behavior
- Pneumocystis jirovecii pneumonia detection and treatment
Johannes Gutenberg University Mainz
2019-2024
Virginia Commonwealth University
2021
University of Applied Sciences Mainz
2020
A two-step route to MK-4482 (EIDD-2801, 1) was developed consisting of an esterification and hydroxamination cytidine.
An efficient gram-scale synthesis of the antituberculosis agent pretomanid using straightforward chemistry, mild reaction conditions, and readily available starting materials is reported. Four different protecting groups on glycidol moiety were investigated for their technical feasibility ability to suppress side reactions. Starting from protected (R)-glycidols 2-bromo-4-nitro-1H-imidazole, could be prepared in a linear three-step up 40% isolated yield. In contrast most syntheses reported so...
A versatile protocol for light induced catalytic activation of thioglycosides using iodine as an inexpensive and readily available photocatalyst was developed. Oxygen serves a green cost‐efficient terminal oxidant irradiation is performed with common household LED‐bulb. The scope this glycosylation investigated in the synthesis O ‐glycosides yields up to 95 %.
Synthetic cannabinoids (SCs) are one of the largest groups new psychoactive substances (NPSs). However, relationship between their chemical structure and affinity to human CB
Carbohydrates such as glucose are an abundant renewable resource that can be employed in synthetic processes a source of carbon and/or hydrogen to yield products high economical and biological impact. Herein, we report versatile environmentally friendly protocol for the one‐pot synthesis 2,3‐dihydroquinazolin‐4(1 H )‐ones, privileged scaffold medicinal chemistry, based on use eco‐friendly reductant alkaline aqueous medium. This method viewed blueprint development further sequences involving...
A short and practical synthesis for preparing the active pharmaceutical ingredient dolutegravir sodium was developed. The convergent strategy starts from (R)-3-amino-1-butanol establishes BC ring system in a 76% isolated yield over four steps. Ring constructed by one-pot 1,4-addition to diethyl-(2E/Z)-2-(ethoxymethylidene)-3-oxobutandioate subsequent MgBr2·OEt2-mediated regioselective cyclization. Amide formation with 2,4-difluorobenzylamine either performed free carboxylic acid or through...
New chemical moieties continue to appear in synthetic cannabimimetics (SC), the largest group of new psychoactive substances EU. We describe first comprehensive characterisation novel SC Cumyl-Tosyl-Indazole-3-Carboxamide (Cumyl-TsINACA) (N-[2-phenylpropan-2-yl]-1-tosyl-1H-indazole-3-carboxamide) from seized case samples. Structure elucidation was performed within EU-project ADEBAR plus facilitate confident identification by other researchers and practitioners worldwide. Characteristic MS...
Bedaquiline is a crucial medicine in the global fight against tuberculosis, yet its high price places it out of reach for many patients. Herein, we describe improvements to key industrial lithiation-addition sequence that enable higher yielding and therefore more economical synthesis bedaquiline. Prioritization mechanistic understanding multi-lab reproducibility led optimized reaction conditions feature an unusual base-salt pairing afford doubling yield racemic We anticipate implementation...
Seven new macrolactones of the oxacyclododecindione family have been synthesized and tested for their inhibitory activity on TGF-β-inducible Smad2/3- as well IL-4-inducible STAT6-dependent signalling pathways.
A two-step route to MK-4482 (EIDD-2801, 1 ) was developed consisting of an esterification and hydroxamination cytidine. The reactions can be conducted in either order with overall yields 67% (first step—esterification) 37% step—hydroxamination). Selective the nucleoside’s primary alcohol by enzymatic means eliminated need for diol protection/deprotection, direct transamination hydroxylamine precluded necessity activating nucleobase amine coupling. This results a significant advancement over...
A synthesis of fluorinated pyrimidines under mild conditions from amidine hydrochlorides and the recently described potassium 2-cyano-2-fluoroethenolate was developed. broad substrate scope tested mostly excellent yields were obtained. The aminopyrazoles same precursor could be demonstrated but proceeded with lower efficiency.
A two-step route to MK-4482 (EIDD-2801, <b>1</b>) was developed consisting of an esterification and hydroxamination cytidine. The reactions can be conducted in either order with overall yields 67% (first step—esterification) 37% step—hydroxamination). Selective the nucleoside’s primary alcohol by enzymatic means eliminated need for diol protection/deprotection, direct transamination hydroxylamine precluded necessity activating nucleobase amine coupling. This results a significant...
Bedaquiline is a crucial medicine in the global fight against tuberculosis, yet its high price places it out of reach for many patients. Herein, we describe improvements to key industrial lithiation-addition sequence that enable higher yielding and therefore more economical synthesis bedaquiline. Prioritization mechanistic understanding multi-lab reproducibility led optimized reaction conditions feature an unusual base–salt pairing afford doubling yield racemic We anticipate implementation...
Synthetic cannabinoid receptor agonists (SCRAs) are distributed on the drug market to produce THC-like effects while evading routine testing and legislation. The cyclobutylmethyl (CBM) norbornylmethyl (NBM) side chain specifically circumvented German legislation led emergence of exploratory SCRAs in 2019-2021. NBM were detected post-amendment new psychoactive substances act 2020, which scheduled all CBM SCRAs. All six full at 1 compared with Δ9 -tetrahydrocannabinol CP-55,940. showed binding...
A short and practical synthesis for preparing the active pharmaceutical ingredient dolutegravir sodium was investigated. The convergent strategy developed herein starts from 3-(R)-amino-1- butanol builds up BC ring system in 76% isolated yield over four steps. Ring constructed by a one-pot 1,4-addition to diethyl-(2E/Z)-2-(ethoxymethylidene)-3-oxobutandioate subsequent MgBr2·OEt2-mediated regioselective cyclization. Amide formation with 2,4- difluorobenzylamine either performed carboxylic...
A short and practical synthesis for preparing the active pharmaceutical ingredient dolutegravir sodium was investigated. The convergent strategy developed herein starts from 3-(R)-amino-1- butanol builds up BC ring system in 76% isolated yield over four steps. Ring constructed by a one-pot 1,4-addition to diethyl-(2E/Z)-2-(ethoxymethylidene)-3-oxobutandioate subsequent MgBr2·OEt2-mediated regioselective cyclization. Amide formation with 2,4- difluorobenzylamine either performed carboxylic...