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A Pd(II)-catalyzed reaction for the direct arylation of cyclic enaminones is reported. The reactivity of electron-rich, electron-poor, and sterically encumbered organotrifluoroborates was investigated. This reaction represents a unique use for organotrifluoroborates as coupling partners and discloses the utility of enaminones for direct-functionalization(More)
The transition-metal-catalyzed direct C-H bond fluorination is an attractive synthetic tool toward the preparation of organofluorines. While many methods exist for the direct sp(3) C-H functionalization, site-selective fluorination of unactivated sp(3) carbons remains a challenge. Direct, highly site-selective and diastereoselective fluorination of(More)
CD14 is a receptor for lipopolysaccharide and plays an important role in innate immune against infections induced by microorganisms. A functional polymorphism in promoter region of CD14 gene, −159C/T, was extensively investigated with tuberculosis (TB) risk, but the association results were inconclusive. We performed a meta-analysis to synthesize(More)
A focused library of TX-67 (C10 hemi-succinate) analogs has been prepared, including C7 regioisomers, esters, amides, and one-carbon homologs. These were prepared to investigate whether the lack of TX-67 interaction with P-glycoprotein (Pgp) is due to the presence of the carboxylic acid moiety and whether this phenomenon was restricted to C10 analogs.(More)
The intramolecular dehydrogenative amidation of aliphatic amides, directed by a bidentate ligand, was developed using a copper-catalyzed sp(3) C-H bond functionalization process. The reaction favors predominantly the C-H bonds of β-methyl groups over the unactivated methylene C-H bonds. Moreover, a preference for activating sp(3) C-H bonds of β-methyl(More)
Intramolecular dehydrogenative cyclization of aliphatic amides was achieved on unactivated sp(3) carbon atoms by a nickel-catalyzed CH bond functionalization process with the assistance of a bidentate directing group. The reaction favors the CH bonds of β-methyl groups over the γ-methyl or β-methylene groups. Additionally, a predominant preference for the(More)
Coumarin and flavone derivatives are highly valuable molecules in drug discovery. Here, two new regioselective cross-dehydrogenation couplings of coumarins and flavones with different ethers via C(sp(3))-H functionalization processes were developed, generating new ether-substituted derivatives not previously reported. These reactions proceeded well via(More)
The direct cyanomethylation of unactivated sp3 C-H bonds of aliphatic amides was achieved via palladium catalysis assisted by a bidentate directing group with good functional group compatibility. This process represents the first example of the direct cross-coupling of sp3 C-H bonds with acetonitrile. Considering the importance of the cyano group in(More)
OBJECTIVE Genome-wide association study (GWAS) recently identified several susceptibility loci in ASAP1 gene on chromosome 8q24 for tuberculosis (TB) in a Russian population, but no relevant studies have been performed to validate these findings. In addition, previous GWAS in Ghana and Gambia found that the variant rs4331426 at 18q11.2 was a susceptibility(More)