1510865-58-3Relevant academic research and scientific papers
Pyrimidine derivative, preparation method therefor and application thereof in medicine
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, (2016/10/07)
The invention relates to a pyrimidine derivative, a preparation method therefor and an application thereof in medicine. Particularly, the invention relates to a compound as shown in general formula (M) or a stereisomer, an aquo-complex, a metabolic product, a solvate, a pharmaceutically acceptable salt, a co-crystallization or a prodrug thereof; the preparation method thereof; and the application of the medicine composition thereof and the compound medicine compound in the medicine, particularly the application as an EGFR target spot inhibitor, wherein the definition of each substituent group in the general formula (M) is the same as that of the specification.
Metal-free coupling of saturated heterocyclic sulfonylhydrazones with boronic acids
Allwood, Daniel M.,Blakemore, David C.,Brown, Alan D.,Ley, Steven V.
, p. 328 - 338 (2014/01/17)
The coupling of aromatic moieties with saturated heterocyclic partners is currently an area of significant interest for the pharmaceutical industry. Herein, we present a procedure for the metal-free coupling of 4-, 5-, and 6-membered saturated heterocyclic p-methoxyphenyl (PMP) sulfonylhydrazones with aryl and heteroaromatic boronic acids. This procedure enables a simple, two-step synthesis of a range of functionalized sp2-sp3 linked bicyclic building blocks, including oxetanes, piperidines, and azetidines, from their parent ketones.
