A5100728555- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthesis of heterocyclic compounds
- Multicomponent Synthesis of Heterocycles
- Chemical Synthesis and Analysis
- Synthesis and biological activity
- Organic Electronics and Photovoltaics
- Organic and Molecular Conductors Research
- Innovative Microfluidic and Catalytic Techniques Innovation
- Synthesis and Properties of Aromatic Compounds
- Catalytic C–H Functionalization Methods
- Asymmetric Synthesis and Catalysis
- Lysosomal Storage Disorders Research
- Synthesis and Biological Activity
- Asymmetric Hydrogenation and Catalysis
- Thermal and Kinetic Analysis
- Chemistry and Chemical Engineering
- Carbohydrate Chemistry and Synthesis
- Polyamine Metabolism and Applications
- Crystallography and molecular interactions
- Plant Gene Expression Analysis
- Oxidative Organic Chemistry Reactions
- Sphingolipid Metabolism and Signaling
- Quinazolinone synthesis and applications
- Chemical Thermodynamics and Molecular Structure
Novartis (Switzerland)
2024
Novartis (China)
2020-2023
University of Minnesota
2012-2018
University of Kansas
2013-2017
University of Minnesota, Duluth
2011
A direct synthesis of new donor materials for organic photovoltaic cells is reported. Diaryindenotetracenes were synthesized utilizing a Kumada-Tamao-Corriu cross-coupling peri-substituted tetrachlorotetracene with spontaneous indene annulation via C-H activation. Vacuum deposited planar heterojunction incorporating these molecules as electron donors exhibit power conversion efficiencies exceeding 1.5% open-circuit voltages ranging from 0.7 to 1.1 V when coupled C(60) an acceptor.
LCZ696 is a novel treatment for patients suffering from heart failure that combines the two active pharmaceutical ingredients sacubitril and valsartan in single chemical compound. While an established drug substance, new manufacturing process suitable large-scale commercial production had to be developed sacubitril. The use of chemocatalysis, biocatalysis, flow chemistry as state-of-the-art technologies allowed efficiently build up structure achieve defined performance targets.
A process using an engineered phenylalanine ammonia lyase (PAL) enzyme was developed as part of alternative route to a key intermediate olodanrigan (EMA401). In the first this report, detailed results from screening for optimal reaction conditions are presented, followed by discussion several workup strategies investigated. PAL-catalyzed reaction, 70–80% conversion cinnamic acid derivative corresponding could be achieved. The subsequently telescoped Pictet–Spengler with formaldehyde, and...
Abstract Analogues of N ‐butyl‐1‐deoxynojirimycin ( B‐DNJ) were prepared and assayed for inhibition ceramide‐specific glucosyltransferase (CGT), non‐lysosomal β‐glucosidase 2 (GBA2) the lysosomal 1 (GBA1). Compounds 5 a – 6 f , which carry sterically demanding nitrogen substituents, compound 13 devoid C3 C5 hydroxy groups present in DNJ/ B‐DGJ ‐butyldeoxygalactojirimycin) showed no inhibitory activity CGT or GBA2. Inversion stereochemistry at C4 ‐( n ‐butyl)‐ ‐nonyl)‐DGJ (compounds 24 ) also...
Electron-deficient asymmetrically substituted diarylindenotetracenes were prepared via a series of Friedel–Crafts acylations, aryl–aryl cross-couplings, and an intramolecular oxidative cyclization to form the indene ring. Single-crystal X-ray experiments showed good π–π overlap with distances ranging from 3.26 3.76 Å. Both thermogravimetric analysis differential scanning calorimetry indicated that indenotetracenes (ASIs) are stable at elevated temperatures. From cyclic voltammetry...
Reactions of N-alkyl-2,3-dihydro-4-pyridones and 4-(pyrrolidin-1-yl)furan-2(5H)-one with aldehydes triethylsilane in a one-flask procedure provided C5 C3 alkylated derivatives, respectively.Mannich-type reactions formaldehyde carbamates the presence lithium perchlorate furnished C5/C3 methylcarbamates.
A hazardous side reaction between N-bromosuccinimide (NBS) and 2-methyltetrahydrofuran (2-MeTHF) was identified during the thermal safety analysis toward a bromination process. delay owing to preferred free-radical initiation observed. The progress of influence NBS concentration on heat were studied by means different calorimeters. flow desired measured calorimeter (RC1), indicating could be controlled under semibatch mode with appropriate feeding program NBS. On basis these investigations,...
The development of a safe, efficient and scalable continuous‐flow‐chemistry protocol for the O‐difluoromethylation two 3‐hydroxypyridine building blocks is described. This example highlights that continuous flow chemistry has become firmly established within Novartis Biomedical Research, when implemented appropriately can enable supply material from first realization potentially interesting intermediate discovery project all way through to clinical evaluation.
A one-flask procedure was developed to prepare C5 alkyl-substituted analogs of N-benzyl-2,3-dihydro-4-pyridones is reported.
Abstract A scalable and environmentally benign route to the free base of branaplam, a small molecule splicing modulator, was identified developed. This alternative approach circumvented inherent risk dioxin formation associated with ortho ‐halo phenol derivatives present in previous route. Friedel–Crafts provided reliable access key intermediate, subsequently followed by Suzuki–Miyaura cross‐coupling. Multiple process aspects synthetic were evaluated, robust for its large‐scale synthesis...