A5047550005- Magnetism in coordination complexes
- Advanced NMR Techniques and Applications
- Cancer-related cognitive impairment studies
- Advanced Breast Cancer Therapies
- Crystallization and Solubility Studies
- Asymmetric Hydrogenation and Catalysis
- Organic and Molecular Conductors Research
- Organoboron and organosilicon chemistry
- X-ray Diffraction in Crystallography
- Cancer therapeutics and mechanisms
- Chemical Synthesis and Analysis
- Chemical Reactions and Mechanisms
- Crystallography and molecular interactions
- Industrial Gas Emission Control
- Coordination Chemistry and Organometallics
- Asymmetric Synthesis and Catalysis
- Organic Electronics and Photovoltaics
- Organic Light-Emitting Diodes Research
- Innovative Microfluidic and Catalytic Techniques Innovation
- Synthesis and Properties of Aromatic Compounds
- Synthesis and properties of polymers
- Polyoxometalates: Synthesis and Applications
- Cancer Treatment and Pharmacology
- Calcium Carbonate Crystallization and Inhibition
- Phenothiazines and Benzothiazines Synthesis and Activities
Eli Lilly (Ireland)
1999-2024
Eli Lilly (United States)
2009-2015
California Institute of Technology
1993
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTPrototypes for the Polaronic Ferromagnet. Synthesis and Characterization of High-Spin Organic PolymersMichael M. Murray, Piotr Kaszynski, David A. Kaisaki, Wonghil Chang, Dennis DoughertyCite this: J. Am. Chem. Soc. 1994, 116, 18, 8152–8161Publication Date (Print):September 1, 1994Publication History Published online1 May 2002Published inissue 1 September...
A batch process was developed to produce 1-(azidomethyl)-3,5-bis-(trifluoromethyl)benzene, 1, in 94% yield by an efficient nucleophilic substitution reaction between 3,5-bis-(trifluoromethyl)benzyl chloride, 4, and sodium azide. Hydrazoic acid (HN3), a toxic volatile compound with explosive properties, can be formed the reactor headspace during conventional processing that requires significant engineering controls. In order improve overall safety profile, azide 1 optimized for operation...
The hazard assessment of a telescoped Miyaura borylation and Suzuki coupling reaction employing bis(pinacolato)diboron (BisPin), used in the developmental synthesis an intermediate for abemaciclib, led to observation hydrogen being generated. Quantitative headspace GC solution 11B NMR were show that rapid decomposition excess BisPin from under aqueous basic conditions was responsible H2 generation. moles observed found equal excess, which is rationalized by mass balance stoichiometric...
A commercial synthesis was developed for the production of (4-benzylmorpholin-2-(S)-yl)-(tetrahydropyran-4-yl)methanone mesylate, 1a, a key starting material phase 2, new investigational drug candidate at Eli Lilly and Company. The target compound produced in clinical pilot plant by combination two steps: resolution morpholine amide intermediate to install S-morpholino stereocenter 35% yield high-yielding (89%) Grignard reaction generate title isolated as mesylate salt. found proceed...
This paper presents a case study in establishing the operation space of Grignard reaction continuous stirred tank reactor (CSTR). The is multivariate with boundary defined by proven acceptable range every CSTR process parameter such as flow rates and temperature. mapping was conducted thorough understanding kinetics, magnesium (Mg) sequestration efficiency, equipment characterization, impact disturbances has on steady state. A fit-for-use kinetics model developed to parametrize mass transfer...
Abstract A number of new organic tetraradicals with quintet ground states have been prepared. Along their intrinsic significance, these structures provide valuable tests certain design principles for the construction magnetic materials. The all follow “bis(TMM)” approach, which promises to a wealth information on spin preferences in structures. Efforts prepare prototypes polaronic ferromagnet are also described. Current work is aimed at evaluating role bipolaron formation such systems, an...
A new synthesis for an intermediate of abemaciclib is described. Keys to this route are the use inexpensive starting materials, biphasic amine alkylation mild C–N bond formation, anhydrous coupling a 2-chloropyridine derivative with LiHMDS avoid hydroxy impurity, and neutral, fluoride-free conditions affect desilylation. Scale-up optimized described on kilogram scale.
Improved reaction conditions have been developed for a telescoped Miyaura borylation/Suzuki coupling process, which is utilized in the synthesis of an abemaciclib intermediate. Key improvements include situ generation lipophilic base and tailored ligand selection each palladium-catalyzed step. Optimizing choice significantly reduced aryl scrambling, major source impurities borylation Additionally, process led to shortened times lower palladium loadings, resulting more efficient,...