5932-30-9Relevant articles and documents
Generation of Diazomethyl Radicals by Hydrogen Atom Abstraction and Their Cycloaddition with Alkenes
Dong, Kuiyong,Doyle, Michael P.,Su, Yong-Liang,Zheng, Haifeng
supporting information, p. 18484 - 18488 (2021/07/20)
A general catalytic methodology for the synthesis of pyrazolines from α-diazo compounds and conjugated alkenes is reported. The direct hydrogen atom transfer (HAT) process of α-diazo compounds promoted by the tert-butylperoxy radical generates electrophilic diazomethyl radicals, thereby reversing the reactivity of the carbon atom attached with the diazo group. The regiocontrolled addition of diazomethyl radicals to carbon-carbon double bonds followed by intramolecular ring closure on the terminal diazo nitrogen and tautomerization affords a diverse set of pyrazolines in good yields with excellent regioselectivity. This strategy overcomes the limitations of electron-deficient alkenes in traditional dipolar [3+2]-cycloaddition of α-diazo compounds with alkenes. Furthermore, the straightforward formation of the diazomethyl radicals provides umpolung reactivity, thus opening new opportunities for the versatile transformations of diazo compounds.
PYRIMIDINONE-CONTAINING COMPOUND, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
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Paragraph 0156; 0158, (2021/01/22)
Disclosed is a pyrimidinone-containing compound represented by formula I, a preparation method thereof, a pharmaceutical composition, and an application thereof. The pyrimidinone-containing compound of the present disclosure can be used as HIV-1 inhibitor
Discovery of Membrane-Bound Pyrophosphatase Inhibitors Derived from an Isoxazole Fragment
Johansson, Niklas G.,Turku, Ainoleena,Vidilaseris, Keni,Dreano, Lo?c,Khattab, Ayman,Ayuso Pérez, Daniel,Wilkinson, Aaron,Zhang, Yuezhou,Tamminen, Matti,Grazhdankin, Evgeni,Kiriazis, Alexandros,Fishwick, Colin W. G.,Meri, Seppo,Yli-Kauhaluoma, Jari,Goldman, Adrian,Boije Af Genn?s, Gustav,Xhaard, Henri
supporting information, p. 605 - 610 (2020/03/10)
Membrane-bound pyrophosphatases (mPPases) regulate energy homeostasis in pathogenic protozoan parasites and lack human homologues, which makes them promising targets in e.g. malaria. Yet only few nonphosphorus inhibitors have been reported so far. Here, w