A5059971471- Chemical Synthesis and Analysis
- Innovative Microfluidic and Catalytic Techniques Innovation
- Cancer therapeutics and mechanisms
- X-ray Diffraction in Crystallography
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Biological Evaluation
- Crystallization and Solubility Studies
- Microbial Natural Products and Biosynthesis
- Biochemical and Molecular Research
- Mass Spectrometry Techniques and Applications
- Analytical Chemistry and Chromatography
- Oxidative Organic Chemistry Reactions
- Marine Sponges and Natural Products
- Antifungal resistance and susceptibility
- Nanomaterials for catalytic reactions
- Pharmacogenetics and Drug Metabolism
- Chemical Synthesis and Reactions
- Advanced Control Systems Optimization
- Advanced Control Systems Design
- Alkaloids: synthesis and pharmacology
- Plant Physiology and Cultivation Studies
- Protein purification and stability
- Fault Detection and Control Systems
- Catalytic Cross-Coupling Reactions
- Porphyrin and Phthalocyanine Chemistry
National Chemical Laboratory
2012-2023
Academy of Scientific and Innovative Research
2020-2023
Virginia Commonwealth University
2021-2022
Nantes Université
2019-2021
Chimie et Interdisciplinarité, Synthèse, Analyse, Modélisation
2019-2021
Centre National de la Recherche Scientifique
2019-2021
University of Richmond
2020
Kerala Agricultural University
2019
Council of Scientific and Industrial Research
2016
Indra (Spain)
2009
A two-step route to MK-4482 (EIDD-2801, 1) was developed consisting of an esterification and hydroxamination cytidine.
A two-step synthesis of molnupiravir (1) is presented. This work focuses on the development practical reaction and purification conditions toward a manufacturing route. The sequence commences from highly available cytidine (2), formed through direct hydroxamination cytosine ring esterification sugar's primary alcohol without use protecting or activating groups. crystalline hydrate N-hydroxycytidine (3) resulted in an easily purified intermediate, practical, off-the-shelf enzyme was selected...
Naturally occurring benzoxanthenones, which belong to the vast family of lignans, are promising biologically relevant targets. They biosynthetically produced by oxidative dimerization 2-propenyl phenols. In this manuscript, we disclose a powerful automated flow-based strategy for identifying and optimizing cobalt-catalyzed oxidizing system bioinspired We designed reconfigurable flow reactor associating online monitoring process control instrumentation. Our machine was first configured as an...
A continuous flow ozonolysis method combined with a multi-step sequence is developed for the synthesis of drug ivacaftor first time.
A total synthesis of Deoxy-solomonamide B was accomplished starting from tryptophan in an efficient manner by mimicking the proposed biogenetic route. The present utilizes a crotylation, oxidative cleavage indole moiety, and macrolactamization as key steps. use nucleus masked anthranilic acid unit paves way for easy related macrocycles natural products where ortho-acyl aniline moiety is embedded into them, which otherwise difficult to synthesize.
Abstract Described herein is a continuous‐flow strategy for the palladium‐catalyzed direct C−H arylation of indole‐3‐acetic acid derivatives with arenediazonium salts. A fully autonomous self‐optimizing flow platform was used to efficiently optimize coupling reaction in three‐dimensional space. The methodology developed experimentally simple, mild, broad scope, and safer than traditional batch approaches. Our approach particularly convenient prepare precursors pharmaceutically relevant...
A first synthetic effort toward total synthesis of highly potent solomonamides is disclosed. An efficient strategy to synthesize this class compounds, along with the a core macrocycle (shown in red) and key fragment AHMOA, described.
Abstract A simple and convenient method to access 4‐quinolone‐3‐carboxylic acid amides from indole‐3‐acetic through one‐pot oxidative cleavage of the indole ring followed by condensation (Witkop–Winterfeldt type oxidation) was explored. The scope confirmed with more than 20 examples successfully applied synthesis drug Ivacaftor, most expensive on market.
Herein, we disclose a facile synthetic strategy to access an important class of drug molecules that contain chiral 1,2-amino alcohol functionality utilizing highly effective ruthenium-catalyzed asymmetric transfer hydrogenation unprotected α-ketoamines. Recently, the COVID-19 pandemic has caused crisis shortage many drugs, especially norepinephrine and epinephrine, for treatment anaphylaxis hypotension because increased demand. Unfortunately, existing technologies are not fulfilling...
MMV390048 (1) is a clinical compound under investigation for antimalarial activity. A new synthetic route was developed which couples two aromatic fragments while forming the central pyridine ring over steps. This sequence takes advantage of raw materials used in existing etoricoxib supply chain and eliminates need palladium catalysts, were projected to be major cost-drivers.
We report a new class of highly effective, benzooxaphosphole-based, water-soluble ligands in the application Suzuki–Miyaura cross-coupling reactions for sterically hindered substrates aqueous media. The catalytic activities coupling were greatly enhanced by addition amounts organic phase transfer reagents, such as tetraglyme and tetrabutylammonium bromide. optimized general protocol can be conducted with low catalyst load, thereby providing practical solution these reactions. viability this...
Solomonamides, a pair of macrocyclic peptide natural products originating from marine sources, have garnered significant attention within the synthetic community owing to their marked anti-inflammatory efficacy and intricate molecular architectures. In this paper, we present very detailed investigation into solomonamides, including challenges associated with total synthesis, evolution our strategies, structural reassignment, synthesis all possible stereoisomeric macrocycles, biological...
A continuous flow synthesis of FGIN-1-27 has been developed using enabling technologies such as real-time in-line benchtop 19 F NMR analysis and an optimization algorithm.
This work illustrates a new control strategy of model predictive for pH the Cephradine purification process in Continuous stirrer tank reactor (CSTR). The simulation results show that response MPC is accurate and nearer to ideal when compared PID.
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 concise and practical synthesis has been developed to provide the 8-fluoro-5-hydroxy-3,4-diydrocarbostyril (
Abstract 4‐Oxoquinoline‐3‐carboxamides are simply and conveniently obtained from 3‐indoleacetamides by one‐pot oxidative cleavage of the indole ring subsequent condensation (Witkop—Winterfeldt oxidation).
Pyrrolo[2,1-f][1,2,4]triazines are important scaffolds in a number of active pharmaceutical ingredients with broad range biological activities to treat broad-spectrum viral infections. We recently reported the synthesis at kilogram scale batch mode extensive process safety studies, where NaH was applied as base deprotonate 2-cyanopyrrole, and then situ prepared monochloramine solution utilized for N-amination, followed by cyclization formamidine acetate produce required...
A concise and practical synthesis has been developed to provide the 8-fluoro-5-hydroxy-3,4-diydrocarbostyril (8-FDC) fragment of OPC-167832 in 41 % yield > 99 purity over 4 steps from 3-amino-4-fluorophenol. The key feature this process is development a telescoped one pot quinolone via chemoselective amidation easier product isolation without need for column chromatography.