A5080960738- Chemical Synthesis and Analysis
- Neuropeptides and Animal Physiology
- Chemical Synthesis and Reactions
- Cancer therapeutics and mechanisms
- Pain Mechanisms and Treatments
- Analytical Chemistry and Chromatography
- Microbial Natural Products and Biosynthesis
- Ionic liquids properties and applications
- Asymmetric Hydrogenation and Catalysis
- Cytokine Signaling Pathways and Interactions
- Carbohydrate Chemistry and Synthesis
- Peptidase Inhibition and Analysis
- Synthesis and Catalytic Reactions
- Crystallization and Solubility Studies
- Radical Photochemical Reactions
- Receptor Mechanisms and Signaling
- X-ray Diffraction in Crystallography
- Synthesis and Biological Evaluation
- Fluorine in Organic Chemistry
- Veterinary Pharmacology and Anesthesia
- Phosphodiesterase function and regulation
- Asymmetric Synthesis and Catalysis
- Chemical Reaction Mechanisms
- Phenothiazines and Benzothiazines Synthesis and Activities
- Carbon dioxide utilization in catalysis
Mirati Therapeutics (United States)
2023
Rowan University
2016-2020
University of Pittsburgh
2018
Novel eco-friendly tetramethylguanidinium propanesulfonic acid trifluoromethylacetate ([TMGHPS][TFA]) ionic liquid was developed as catalyst and medium for the Fischer indole synthesis of a wide variety hydrazines ketones. The products were isolated in high yields with minimal amounts organic solvent. This reaction showed that [TMGHPS][TFA] can be regenerated reused reproducible without eroding integrity liquid.
The "butterfly-shaped" bicyclic pyrrolidinol ((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)-methanol (1) is a key building block for drug candidates, and its practical chemical synthesis remains elusive. As such, an asymmetric that amenable scale-up has been developed. newly optimized process utilizes readily available N-Boc-trans-4-hydroxy-l-proline methyl ester (8) to establish the challenging stereogenic center bearing fluoride. Subsequent diastereoselective α-alkylation was...
MRTX0902, a novel SOS1 inhibitor, is currently being evaluated in phase I trials for the treatment of cancer. The complexity molecule, which contains pyrido[3,4-d]pyridazine core and chiral amine moiety, makes it challenging target to prepare on multi-kilogram scale support clinical development studies. An efficient scalable synthesis key intermediate 4-methyl-7-morpholinopyrido[3,4-d]pyridazin-1(2H)-one much improved end-game MRTX0902 were developed.
An efficient synthesis of β-amino alcohols from a variety epoxides and primary unbranched amines in the absence any catalyst high yields regioselectivities is reported. A polar mixed solvent systems allow for selective formation secondary amino over tertiary alcohols. The reaction scope extends to wide aromatic aliphatic substituted bearing complex functionality.
The 2,2,6,6-tetramethylpiperidin-1-yloxycarbonyl (Tempoc) protecting group is readily introduced by the reaction of amines with a new acyl transfer reagent, 4-nitrophenyl (2,2,6,6-tetramethylpiperidin-1-yl) carbonate (NPTC). Tempoc has reactivity profile that complements commonly used t-butyloxycarbonyl (Boc) and benzyloxycarbonyl (Cbz) groups. Deprotection can be achieved under mild reductive conditions in situ generated Cu(I) species or thermolytic cleavage at 135 °C. Mechanistic studies...
IBNtxA (3-iodobenzoyl naltrexamine) is a novel μ-opioid receptor (MOR) agonist which structurally related to the MOR antagonist naltrexone. Recent studies suggest preferentially signals through truncated splice variants, resulting in anti-nociception with reduced side effects, including no conditioned place preference (CPP) when tested at single dose. represents an intriguing lead compound for preclinical drug development targeting but further evaluation of its
Cyanopyrrolidinyl β‐amino alcohols are novel scaffolds with potential for a wide array of pharmacological properties. We have discovered that we can selectively access these from simple and inexpensive commercially available chemicals in few synthetic steps minimal purification. produced 36‐compound library tested them as dipeptidyl peptidase IV (DPP4) inhibitors. These inhibitors useful the treatment diabetes inflammatory disorders.
CHCl3 4-nitrophenyl (2,2,6,6-tetramethylpiperidin-1-yl
MRTX0902, a novel SOS1 inhibitor, is currently being evaluated in phase I trials for the treatment of cancer. The complexity molecule containing pyrido[3,4-d]pyridazine core and chiral amine moiety makes it challenging target to prepare on multi-kilogram scale support clinical development studies. An efficient scalable synthesis key intermediate, 4-methyl-7-morpholinopyrido[3,4-d]pyridazin-1(2H)-one much improved end-game MRTX0902 was developed.
ABSTRACT Rationale IBNtxA (3-iodobenzoyl naltrexamine) is a novel μ opioid receptor (MOR) agonist structurally related to the classical MOR antagonist naltrexone. Recent studies suggest preferentially signals through truncated splice variants, producing unique pharmacological profile resulting in antinociception with reduced side effects, including no conditioned place preference (CPP) when tested at single dose. represents an intriguing lead compound for preclinical drug development...