700811-29-6Relevant articles and documents
Preparation method of 2-chloro-4-hydrazinopyridine
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Paragraph 0023-0029, (2019/08/06)
The invention discloses a synthetic method of 2-chloro-4-hydrazinopyridine. The synthetic method is characterized in that the method includes the following steps: dispersing 4-bromo-2-chloropyridine in hydrazine hydrate for reaction at 20-60 DEG C for 12-48 h, and adjusting the pH to alkaline to obtain the 2-chloro-4-hydrazinopyridine. The synthetic method of the 2-chloro-4-hydrazinopyridine of the invention has the advantages of simple operation steps, mild reaction process and small solid waste pollution. Meanwhile, the 4-bromo-2-chloropyridine raw material is cheap and easily available, andatomic availability is better than corresponding iodides. Moreover, the preparation method of the 2-chloro-4-hydrazinopyridine is simple in process and high in yield, does not need column chromatography for the product, significantly reduces the production cost, and is suitable for large-scale preparation of the 2-chloro-4-hydrazinopyridine.
HETEROARYLS AND USES THEREOF
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Paragraph 0887, (2013/07/05)
This invention provides compounds of formula IB: and also provides compounds of formulas ID, IIB, VB, and IIC: wherein HY, R1, R2, G5, G6, G7, G8, and G9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
Microwave-enhanced nucleophilic fluorination in the synthesis of fluoropyridyl derivatives of [3,2-c]pyrazolo-corticosteroids, potential glucocorticoid receptor-mediated imaging agents
Kahn, Michael G.C.,Konde, Emmanuel,Dossou, Francis,Labaree, David C.,Hochberg, Richard B.,Hoyte, Robert M.
, p. 3454 - 3458 (2007/10/03)
Fluoropyridyl derivatives of [3,2-c]pyrazolo-corticosteroids have high affinity for the glucocorticoid receptor (GR) and are highly active glucocorticoids. They are thus considered to be excellent candidates for PET imaging of GR containing tissues when labeled with fluorine-18 (t1/2 = 110 min). Previously reported syntheses of these fluorinated glucocorticoids were accomplished by conventional thermal nucleophilic halogen exchange reactions with chloropyridyl precursors. These reactions were found to proceed at rates too slow for feasible application to radiosynthesis using [18F]fluoride. We have applied microwave-heating methods to these reactions and found that significant rate enhancements can be realized. Kinetic experiments showed an average relative rate ratio of 3/1 for microwave versus conventional heating and preparative experiments showed an average relative conversion ratio of 4.5/1 during the initial 120 min, a period approximating one half-life of the isotope. The microwave method described was used to prepare previously unreported 2′-(2-fluoro-4-pyridyl)-11β,17,21-trihydroxy-16α-methyl-20-oxo-pregn-4-eno-[3,2-c]-pyrazole, which was evaluated for biological activity.
ACYCLIC PYRAZOLE COMPOUNDS FOR THE INHIBITION OF MITOGEN ACTIVATED PROTEIN KINASE-ACTIVATED PROTEIN KINASE-2
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Page/Page column 236, (2008/06/13)
Compounds are described which inhibit mitogen activated protein kinase-activated protein kinase-2 (MK-2). Methods of making such compounds are described, as well as a method of using them for the inhibition of MK-2, and for the prevention or treatment of a disease or disorder that is mediated by TNFalpha, where the method involves administering to the subject an MK-2 inhibiting compound of the present invention. Pharmaceutical compositions and kits which contain the present MK-2 inhibiting compounds are also described.