A highly efficient procedure was developed for the microwave-assisted synthesis of N-heteroaryl-4-(2-chloroethyl)piperazines and N-heteroaryl-4-(2-chloroethyl)piperidines. Microwave irradiation of electron deficient heteroaryl chlorides with 1,4-diazabicyclo[2.2.2]octane (DABCO) at 160 degrees C for 15 min led to N-heteroaryl-4-(2-chloroethyl)piperazines in good to excellent yields. In a similar manner, microwave irradiation of electron deficient heteroaryl chlorides with quinuclidine at 180 degrees C for 15 min provided N-heteroaryl-4-(2-chloroethyl)piperidines in good to excellent yields. Extension of the method was demonstrated by the development of a one-pot, two-step microwave-assisted protocol for the synthesis of 4-(2-acetoxyethyl)-substituted N-heteroarylpiperazines and N-heteroarylpiperidines to demonstrate the production of a small library in a parallel fashion.
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Org Lett
January 2025
Pfizer Oncology Medicinal Chemistry, San Diego, California 92121, United States.
Sulfonamides are prevalent functional groups represented in both natural and pharmaceutical products. The synthesis of sulfonamides is often straightforward when using nucleophilic amines and electrophilic sulfonyl chlorides. When reactivity challenges arise for nontraditional substrates, harsh conditions or new synthetic routes may be required.
View Article and Find Full Text PDFJ Exp Bot
January 2025
Heinrich Heine University Düsseldorf, Universitätsstraße 1, 40225 Düsseldorf, Germany.
In nature, environmental conditions strongly fluctuate, frequently subjecting plants to periods of immediate photo-oxidative stress. The small molecule ascorbate allows plants to cope with such stress conditions. Ascorbate scavenges reactive oxygen species and enables the rapid and full induction of photoprotective non-photochemical quenching (NPQ).
View Article and Find Full Text PDFBioconjug Chem
January 2025
Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104-5127, United States.
Red blood cells (RBCs) serve as natural transporters and can be modified to enhance the pharmacokinetics and pharmacodynamics of a protein cargo. Affinity targeting of Factor IX (FIX) to the RBC membrane is a promising approach to improve the (pro)enzyme's pharmacokinetics. For RBC targeting, purified human FIX was conjugated to the anti-mouse glycophorin A monoclonal antibody Ter119.
View Article and Find Full Text PDFInorg Chem
January 2025
Institute of Solid State Physics, TU Wien, A-1040 Vienna, Austria.
A novel ternary boride, NiPtB ( = 0.5), was obtained by argon-arc melting of the elements followed by annealing at 750 °C. It exhibits a new structure type with the space group ( = 2.
View Article and Find Full Text PDFPhysiol Plant
January 2025
College of Life Sciences, Nanjing Agricultural University, Nanjing, China.
Phosphorus (P) deficiency is a critical factor limiting crop productivity, primarily due to its detrimental effects on photosynthesis and dry matter accumulation. In this study, we investigate the role of the rice gene OsPHT2;1 in mediating chloroplast P homeostasis and its subsequent impact on photosynthetic function under low P conditions. Stomatal conductance is typically positively correlated with net photosynthetic rates; however, P deficiency disrupts this relationship, leading to reduced stomatal opening and diminished photosynthetic efficiency.
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