A5076208181- Crystallization and Solubility Studies
- Asymmetric Synthesis and Catalysis
- X-ray Diffraction in Crystallography
- Asymmetric Hydrogenation and Catalysis
- Antibiotics Pharmacokinetics and Efficacy
- Cyclopropane Reaction Mechanisms
- Chemical synthesis and alkaloids
- Carbohydrate Chemistry and Synthesis
- Analytical Methods in Pharmaceuticals
- Pharmacological Effects and Toxicity Studies
- Synthetic Organic Chemistry Methods
- Inflammatory mediators and NSAID effects
- Organophosphorus compounds synthesis
- Drug Transport and Resistance Mechanisms
- thermodynamics and calorimetric analyses
- Metabolism and Genetic Disorders
- Helicobacter pylori-related gastroenterology studies
- Biochemical and Molecular Research
- Chemical Synthesis and Analysis
- Catalytic C–H Functionalization Methods
- Pharmacogenetics and Drug Metabolism
- Cancer therapeutics and mechanisms
Shanghai Institute of Organic Chemistry
2009-2014
Chinese Academy of Sciences
2009
United States Military Academy
1977-1982
Merck & Co., Inc., Rahway, NJ, USA (United States)
1978
Merck (France)
1977
The disposition of sulindac, a new nonsteroid anti‐inflammatory drug, has been studied in normal volunteers five separate clinical studies. Based upon material balance considerations, minimum approximately 88% an oral dose is absorbed. major biotransformations involve irreversible oxidation the sulfinyl group sulindac to sulfone and reduction corresponding sulfide. latter, which all available evidence indicates be pharmacologically active form not excreted urine, apparent terminal half‐life...
The kinetic resolution of a carbon nucleophile is realized for the first time via Pd-catalyzed asymmetric allylic alkylation with "unstabilized" ketone enolates as nucleophile, providing both allylated 2,3-disubstituted 2,3-dihydro-4-quinolones and recovered substrates in high yields ee (S-factor 40-145). application methodology organic synthesis demonstrated by ready transformation an adduct into pyrrolo[3,2-c]quinoline, which features core structure biologically active Martinella alkaloids.
α-Carbanions of cyclic and acyclic imines have been successfully applied as nucleophiles in the Pd-catalyzed allylic alkylation reaction. Tuning chemo- regioselectivity has realized by using t-BuOK/THF LDA/toluene to give branched linear products, respectively, with high regio- diastereoselectivities. A plausible mechanism is proposed on basis experimental results DFT calculations.
Phosphonamidate 3a of methoxymethylphosphonic acid (MMPA) with propofol (1) and l-alanine ethyl ester was found to be an efficient scaffold for the oral delivery compound 1. The synthesis evaluation MMPA based phosphonamidates 1, HSK3486 (2), other phenolic drugs revealed general application as effective vehicle drugs. On basis plasma concentrations 1 SN38 (14), bioavailability 15 in beagle dogs 97.6% 34.1%, respectively.
The kinetic resolution of 2-substituted-2,3-dihydro-4-pyridones was realized via a Pd-catalyzed allylic substitution reaction using commercially available (S)-P-Phos as ligand, affording optically active dihydropyridones and C-allylated in high yields good enantioselectivities with the S-factor up to 43. With this protocol, catalytic asymmetric total synthesis indolizidine (−)-209I for first time.
Cyclobenzaprine was extensively metabolized in man, less than 1% of the dose being excreted unchanged urine. Comparison areas under plasma level curves (AUC) after oral and intravenous doses suggests that drug may be partly lumen or during its first passage through gut wall and/or liver. Average levels increased with increasing dosage, but AUC rapidly dose, possibly because dose-dependent absorption.
Abstract The effect of sustained release on the pharmacokinetic profile indomethacin was examined by comparing to three reference regimens: an intravenous dose, a single 75 mg dose conventional capsules, and 25 doses given at 4‐h intervals. Results indicate that test formulation exhibited more prolonged uniform absorption rate, yielded plasma levels after ingestion, showed overall bioavailability 0.93 (95 per cent C.I. = 0.82, 1.04) relative capsules.
Abstract The chemo‐ and regioselectivity in the Pd‐catalyzed allylic alkylation can be tuned by using bases with different counterions.
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