A5094028807- Fluorine in Organic Chemistry
- Asymmetric Hydrogenation and Catalysis
- Chemical Synthesis and Analysis
- PI3K/AKT/mTOR signaling in cancer
- Cancer-related Molecular Pathways
- Coordination Chemistry and Organometallics
- Synthetic Organic Chemistry Methods
- Organometallic Complex Synthesis and Catalysis
- Chronic Lymphocytic Leukemia Research
Mirati Therapeutics (United States)
2024
Chiral amine synthesis remains a significant challenge in accelerating the design cycle of drug discovery programs. A zirconium hydride, due to its high oxophilicity and lower reactivity, gave highly chemo- stereoselective reductions sulfinyl ketimines. The development this zirconocene-mediated reduction helped accelerate our efforts is applicable several motifs commonly used medicinal chemistry. Computational investigation supported cyclic half-chair transition state rationalize selectivity...
The H1047R mutation of PIK3CA is highly prevalent in breast cancers and other solid tumors. Selectively targeting PI3KαH1047R over PI3KαWT crucial due to the role that plays normal cellular processes, including glucose homeostasis. Currently, only one PI3KαH1047R-selective inhibitor has progressed into clinical trials, while three pan mutant (H1047R, H1047L, H1047Y, E542K, E545K) selective PI3Kα inhibitors have also reached stage. Herein, we report design discovery a series...
In our drug discovery campaigns to target the oncogenic drivers of cancers, demand for a chemoselective, stereoselective and economical synthesis chiral benzylamines drove development catalytic zirconium hydride reduction. This methodology uses inexpensive, bench stable zirconocene dichloride, novel tetrabutylammonium fluoride activa-tion tactic catalytically generate metal under ambient conditions. The diastereo- chemoselectivity this reaction was tested with preparation key intermediates...
In our drug discovery campaigns to target the oncogenic drivers of cancers, demand for a chemoselective, stereoselective and economical synthesis chiral benzylamines drove development catalytic zirconium hydride reduction. This methodology uses inexpensive, bench stable zirconocene dichloride, novel tetrabutylammonium fluoride activation tactic catalytically generate metal under ambient conditions. The diastereo- chemoselectivity this reaction was tested with preparation key intermediates...