22 research outputs found
Palladium-mediated in situ synthesis of an anticancer agent
Biocompatible heterogeneous Pd(0) catalysts were used in a Suzuki–Miyaura cross-coupling reaction to synthesise an anticancer agent in situ, leading to apoptosis of prostate cancer cells.</p
Highly selective and rapidly activatable fluorogenic Thrombin sensors and application in human lung tissue
Intracellular delivery of a catalytic organometallic complex
A homogeneous carbene-based palladium catalyst was conjugated to a cell-penetrating peptide, allowing intracellular delivery of catalytically active Pd complexes that demonstrated bioorthogonal activation of a profluorophore within prostate cancer cells
High fidelity fibre-based physiological sensing deep in tissue
Physiological sensing deep in tissue, remains a clinical challenge. Here a
flexible miniaturised sensing optrode providing a platform to perform minimally
invasive in vivo in situ measurements is reported. Silica microspheres
covalently coupled with a high density of ratiometrically configured
fluorophores were deposited into etched pits on the distal end of a 150 micron
diameter multicore optical fibre. With this platform, multiplexed photonic
measurements of pH and oxygen concentration with high precision in the distal
alveolar space of the lung is reported. We demonstrated the phenomenon that
high-density deposition of carboxyfluorescein covalently coupled to silica
microspheres shows an inverse shift in fluorescence in response to varying pH.
This platform delivered fast and accurate measurements, near instantaneous
response time, no photobleaching, immunity to power fluctuations and a flexible
architecture for addition of multiple sensors
In situ identification of Gram-negative bacteria in human lungs using a topical fluorescent peptide targeting lipid A
HClO<SUB>4</SUB>–SiO<SUB>2</SUB> as a new, highly efficient, inexpensive and reusable catalyst for N-tert-butoxycarbonylation of amines
Perchloric acid adsorbed on silica-gel (HClO4–SiO2) was found to be a new, highly efficient, inexpensive and reusable catalyst for chemoselective N-tert-butoxycarbonylation of amines at room temperature and under solvent-free conditions
Copper(II) tetrafluoroborate as a novel and highly efficient catalyst for N-tert-butoxycarbonylation of amines under solvent-free conditions at room temperature
Commercially available copper(II) tetrafluoroborate hydrate was found to be a highly efficient catalyst for chemoselective N-tert-butoxycarbonylation of amines with di-tert-butyl dicarbonate under solvent-free conditions and at room temperature. Various aromatic amines were protected as their N-tert-butyl carbamates in high yields and in short times. No competitive side reactions such as isocyanate, urea, and N,N-di-t-Boc formation was observed. Chemoselective N-tert-butoxycarbonylation was achieved with substrates bearing OH and SH groups. Chiral α-amino acid esters afforded the corresponding N-t-Boc derivatives in excellent yields
Counterattack mode differential acetylative deprotection of phenylmethyl ethers: applications to solid phase organic reactions
A counterattack protocol for differential acetylative cleavage of phenylmethyl ether has been developed. The phenylmethyl moiety is liberated as benzyl bromide that is isolated and reused providing advantages in terms of waste minimization/utilization and atom economy. The applicability of this methodology has been extended for solid phase organic reactions with the feasibility of reuse of the solid support
Catalyst-free chemoselective N-tert-butyloxycarbonylation of amines in water
Catalyst-free N-tert-butyloxycarbonylation of amines in water is reported. The N-t-Boc derivatives were formed chemoselectively without any isocyanate, urea, N,N-di-t-Boc, and O/S-t-Boc as side products. Chiral amines, esters of α-amino acids, and β-amino alcohol afforded optically pure N-t-Boc derivatives. Amino alcohol and 2-aminophenol afforded the N-t-Boc derivative without oxazolidinone formation. Selectivity was observed during competition of aromatic amine vs aliphatic amine, amine vs amino acid ester, amine vs amino alcohol, and primary amine vs secondary amine