888720-29-4Relevant academic research and scientific papers
Deaminative chlorination of aminoheterocycles
Ghiazza, Clément,Faber, Teresa,Gómez-Palomino, Alejandro,Cornella, Josep
, p. 78 - 84 (2021/12/23)
Selective modification of heteroatom-containing aromatic structures is in high demand as it permits rapid evaluation of molecular complexity in advanced intermediates. Inspired by the selectivity of deaminases in nature, herein we present a simple methodology that enables the NH2 groups in aminoheterocycles to be conceived as masked modification handles. With the aid of a simple pyrylium reagent and a cheap chloride source, C(sp2)?NH2 can be converted into C(sp2)?Cl bonds. The method is characterized by its wide functional group tolerance and substrate scope, allowing the modification of >20 different classes of heteroaromatic motifs (five- and six-membered heterocycles), bearing numerous sensitive motifs. The facile conversion of NH2 into Cl in a late-stage fashion enables practitioners to apply Sandmeyer- and Vilsmeier-type transforms without the burden of explosive and unsafe diazonium salts, stoichiometric transition metals or highly oxidizing and unselective chlorinating agents. [Figure not available: see fulltext.]
Novel synthesis method of compound 7-iodopyrrolo[2, 1-f][1, 2, 4]triazin-4-amine
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Paragraph 0046-0048, (2021/09/04)
The invention provides a method for preparing a triazine compound as shown in a formula (I). According to the invention, pyruvic acid and formamidine are taken as starting materials to synthesize an intermediate, and the intermediate is subjected to two-step reaction to obtain the compound shown in the formula (I). The method provided by the invention is mild in condition, simple and convenient to operate, capable of greatly reducing the cost and suitable for industrial mass production.
IMIDAZOTRIAZINE DERIVATIVES AS CD73 INHIBITORS
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Paragraph 0162, (2020/10/28)
The present disclosure relates generally to imidazotriazine derivatives that are inhibitors of CD73 and are useful in treating CD73-associated diseases or conditions. Compositions containing the compounds of the present disclosure are also provided.
BICYCLIC ETHER O-GLYCOPROTEIN-2-ACETAMIDO-2-DEOXY-3-D-GLUCOPYRANOSIDASE INHIBITORS
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Paragraph 00232, (2020/08/22)
Described herein are compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, X, R1, R3, R 4, Y1, Y2, n and p are as defined herein.
Novel compound for preparing key intermediate of remdesivir and preparation method thereof
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Paragraph 0022, (2020/06/24)
The invention relates to a novel compound II used for synthesizing a key intermediate of remdesivir and a preparation method thereof. The preparation method of the compound II comprises the followingsteps: (a) halogenating 4-X-pyrrole[2,1-f][1,2,4]triazine as shown in a formula (V) to obtain 4-X-7-halogenated-pyrrole[2,1-f][1,2,4]triazine as shown in a formula (IV); (b) adding magnesium or alkylmagnesium halide to react with a ribose lactone derivative shown in the formula (VI) to generate glycosylate shown in the formula (III); and (c) converting hydroxyl into cyano in a proper solvent by the glycosylate (III) under the action of a cyaniding agent, a Lewis acid and a Bronsted acid to obtain the compound II. The prepared compound can be used for generating a key intermediate I required in synthesis of remdesivir through an ammoniation reaction. The invention provides a new compound II and a process route which is different from the prior art, is high in reaction selectivity and can be used for preparing the remdesivir key intermediate in batches.
PYRROLOTRIAZINE KINASE INHIBITORS
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Page/Page column 106, (2015/04/28)
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
HETEROCYCLIC COMPOUNDS AS JANUS KINASE INHIBITORS
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, (2013/03/28)
The invention provides compounds of formula I: (I) or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing com-pounds of formula I, intermediates useful for preparing com-pounds of formula I and therapeutic methods for suppressing an immune response or treating cancer, including a hematologic malignancy, using compounds of formula I
HETEROCYCLIC COMPOUNDS AS JANUS KINASE INHIBITORS
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, (2011/12/14)
The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula I.
HETEROCYCLIC COMPOUND AS PROTEIN KINASE INHIBITOR
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Page/Page column 32, (2011/08/06)
Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
THERAPEUTIC AGENTS
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Page/Page column 29;35, (2010/04/03)
The invention provides a compound of formula (I): wherein R1, and W have any of the values defined in the application; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).
