131067-76-0Relevant articles and documents
Aminopyridyloxypyrazole derivative and preparation method and application thereof
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Paragraph 0075; 0382-0387, (2021/05/19)
The invention relates to an aminopyridyloxypyrazole derivative and a preparation method and application thereof. The structure of the aminopyridyloxypyrazole derivative is shown as a formula (I). The invention provides a brand-new aminopyridyloxypyrazole derivative which has obvious effects of inhibiting TGF [beta] R1 (ALK5) kinase activity and treating cancer or fibrosis related diseases, and the preparation method of the derivative is simple and easy to operate.
Selective α-Methylation of Ketones
Frolov, Andriy I.,Ostapchuk, Eugeniy N.,Pashenko, Alexander E.,Chuchvera, Yaroslav O.,Rusanov, Eduard B.,Volochnyuk, Dmitriy M.,Ryabukhin, Sergey V.
, p. 7333 - 7346 (2021/06/28)
The convenient and scalable preparative approach for the two-step α-methylation of ketones is described. The optimized protocols for regioselective preparation of enaminones with further diastereoselective and functional groups tolerant hydrogenation to α-methylketones are developed. The scope and limitations of the proposed methodology are discussed. The advantages compared to known procedures are demonstrated. The unexpected role of acetone in the hydrogenation is suggested. The evaluation of the method for both early building block synthesis and late-stage CH-functionalization is shown. The elaborate procedures' preparability and scalability are demonstrated by the synthesis of several α-methyl ketones up to 100 g amount.
Chemoselective Oxidation of Equatorial Alcohols with N-Ligated λ3-Iodanes
Mikhael, Myriam,Adler, Sophia A.,Wengryniuk, Sarah E.
supporting information, p. 5889 - 5893 (2019/08/26)
The site-selective and chemoselective functionalization of alcohols in complex polyols remains a formidable synthetic challenge. Whereas significant advancements have been made in selective derivatization at the oxygen center, chemoselective oxidation to the corresponding carbonyls is less developed. In cyclic systems, whereas the selective oxidation of axial alcohols is well known, a complementary equatorial selective process has not yet been reported. Herein we report the utility of nitrogen-ligated (bis)cationic λ3-iodanes (N-HVIs) for alcohol oxidation and their unprecedented levels of selectivity for the oxidation of equatorial over axial alcohols. The conditions are mild, and the simple pyridine-ligated reagent (Py-HVI) is readily synthesized from commercial PhI(OAc)2 and can be either isolated or generated in situ. Conformational selectivity is demonstrated in both flexible 1,2-substituted cyclohexanols and rigid polyol scaffolds, providing chemists with a novel tool for chemoselective oxidation.
Preparation method and application of key intermediate of non-opioid analgesic
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Paragraph 0054; 0055; 0064; 0065; 0090; 0091, (2019/08/01)
Dihydro-4-acetal-2H-pyran-3(4H)-one (compound II) is used as a raw material, and the raw material and methyltriphenylphosphine bromide are subjected to a Wittig reaction to obtain a compound III; thedouble bond of the compound III is subjected to a reduction reaction to obtain a compound IV; the compound IV is subjected to acetal hydrolysis under the action of a dilute acid to generate a compoundV; the compound V and benzylamine are subjected to nucleophilic addition reaction to generate a compound VI; and finally, debenzylating and hydrochloride forming are carried out, so that a non-opioidanalgesic key intermediate is obtained, namely cis-3-methyl-4-aminotetrahydropyran hydrochloride (compound I). The method is easy and convenient to operate and high in yield, the total yield can reach 40%, and rapid preparation in a laboratory can be achieved.
AMINO-QUINOLINES AS KINASE INHIBITORS
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Page/Page column 60; 61, (2018/06/22)
Disclosed are compounds having the formula:wherein R 1 , R 2 , R 3 and Z are as defined herein, and methods of making and using the same.
NRF2 ACTIVATOR
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Page/Page column 120, (2018/07/29)
Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.
AMINO-QUINOLINES AS KINASE INHIBITORS
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Page/Page column 70; 71, (2018/05/15)
Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
ANTI-BACTERIAL COMPOUNDS
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Page/Page column 115, (2017/06/28)
A compound of Formula (II): for use in the prevention or treatment of a bacterial infection.
AMINO-QUINOLINES AS KINASE INHIBITORS
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Paragraph 0129, (2016/10/31)
Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
TBK/IKK INHIBITOR COMPOUNDS AND USES THEREOF
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Paragraph 0330; 0331, (2017/01/23)
The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
