90685-58-8Relevant academic research and scientific papers
Visible-Light-Induced ortho-Selective Migration on Pyridyl Ring: Trifluoromethylative Pyridylation of Unactivated Alkenes
Jeon, Jinwon,He, Yu-Tao,Shin, Sanghoon,Hong, Sungwoo
supporting information, p. 281 - 285 (2019/11/26)
The photocatalyzed ortho-selective migration on a pyridyl ring has been achieved for the site-selective trifluoromethylative pyridylation of unactivated alkenes. The overall process is initiated by the selective addition of a CF3 radical to the alkene to provide a nucleophilic alkyl radical intermediate, which enables an intramolecular endo addition exclusively to the ortho-position of the pyridinium salt. Both secondary and tertiary alkyl radicals are well-suited for addition to the C2-position of pyridinium salts to ultimately provide synthetically valuable C2-fluoroalkyl functionalized pyridines. Moreover, the method was successfully applied to the reaction with P-centered radicals. The utility of this transformation was further demonstrated by the late-stage functionalization of complex bioactive molecules.
MITOCHONDRIAL INHIBITORS FOR THE TREATMENT OF PROLIFERATION DISORDERS
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Page/Page column 75, (2019/05/02)
The invention provides compounds of formula (I) or pharmaceutically acceptable salt thereof wherein ring A represents group A-I, A-II or A-III. Al represents -C(R4a)(R4a)-, -C(R4a)= -N(R4b)-, -N= -O- or -S-; A2 represents -C(R4c)(R4c)-, -C(R4c)= or -0-; A3 represents -C(R4c)(R4c)-, -C(R4c)= or -0-; A4 represents -C(R4a)(R4a)-, -C(R4a)= -N= -O- or -S-; A5 represents -C(R4a)(R4a)-, -C(R4a)= -N(R4b)-, -N= -O- or -S-; A6 represents -C(R4c)(R4c)- or -C(R4c)=; A7 represents -C(R4a)(R4a)-, -C(R4a)= -N= -O- or -S-; A8 represents -C(R4a)(R4a)-, -N(R4b)-, -O- or -S-; A9 represents -C(R4c)(R4c)- or -0-; A10 represents -C(R4c)(R4c)- or -0-; A11 represents -C(R4c)(R4c)- or -0-; A12 represents -C(R4a)(R4a)-, -O- or -S-; wherein group A-I, group A-II and group A-III de not contain adjacent oxygen atoms, adjacent oxygen and sulfur atoms or adjacent oxygen and nitrogen atoms or a moiety selected from the group consisting of N-C-N, N-C-S, S-C-S, O-C-N, O-C-O and O-C-S, wherein in each case the carbon atom in the N-C-N, N-C-S, S-C-S, O-C-N, O-C-O and O-C-S moiety is saturated; B1, B2, B3 and B4 represent independently C(R3) or N, wherein no more than two of B1, B2, B3 and B4 represent N; n is 1 or 2; and R1, R2, R3, R4a, R4b and R4c are as defined in the claims, as well as methods of using the compounds to treat proliferation diseases, in particular cancer.
Visible-Light-Induced C2 Alkylation of Pyridine N-Oxides
Zhang, Wen-Man,Dai, Jian-Jun,Xu, Jun,Xu, Hua-Jian
, p. 2059 - 2066 (2017/02/26)
A photoredox catalytic method has been developed for the direct C2 alkylation of pyridine N-oxides. This reaction is compatible with a range of synthetically relevant functional groups for providing efficient synthesis of a variety of C2-alkylated pyridine N-oxides under mild conditions. Mechanistic studies are consistent with the generation of a radical intermediate along the reaction pathway.
Cyclic gyrase and topoisomerase IV inhibitor
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Paragraph 0155; 0156; 0157, (2017/01/02)
The invention belongs to the technical field of medicament, and particularly relates to a compound shown in formula (I) (please see the formula (I) in the description), and acceptable salt, ester or stereoisomer of the compound in pharmacy. R1, R2, a ring
PYRIDINEAMINE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
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Page/Page column 195, (2016/12/22)
The present disclosure describes pyridineamine compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer, immune disorders and other diseases. Formula (I).
FACTOR XIa INHIBITORS
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Page/Page column 38, (2016/11/02)
The present invention provides a compound of Formula (I); and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Enantiopure synthesis of 7-(1-pyrindanyl)propargyl ethers as rasagiline analogues via chemical or enzymatic resolution of 1-pyrindan-7-ol
Sousa, Carlos A. D.,Sampaio-Dias, Ivo E.,Rizzo-Aguiar, Fabio,Garcia-Mera, Xerardo,Rodríguez-Borges, José E.
, p. 104509 - 104515 (2015/12/24)
In this work, the enantiopure synthesis of 7-(1-pyrindanyl)propargyl ethers - rasagiline analogues - via chemical and/or enzymatic resolution of the racemic precursor 1-pyrindan-7-ol is described. (R)-Methoxyphenylacetic acid - (R)-MPAA - and (S)-methoxyphenylacetic acid - (S)-MPAA were used as chemical resolution agents, whereas Candida antarctica lipase B (CALB) was employed as kinetic resolution catalyst. The enzymatic resolution was successfully achieved by two different approaches: (1) transesterification of racemic 1-pyrindan-7-ol, which was found to selectively acylate the (R)-enantiomer with high efficiency; (2) hydrolysis of the racemic 7-(1-pyrindanyl)acetate, which was also highly selective to the (R)-enantiomer. The enzymatic hydrolysis was performed in a non-aqueous solvent using a lipase with significant absorbed water content. The configuration of the two enantiomers of 1-pyrindan-7-ol (and consequently of the 7-(1-pyrindanyl)propargyl ethers) were unequivocally determined by X-ray crystallography and/or specific optical rotation.
Organocatalysts with carbon-centered activity for CO2 reduction with boranes
Yang, Yanxin,Xu, Maotong,Song, Datong
supporting information, p. 11293 - 11296 (2015/07/07)
We report two organocatalysts for CO2 hydroboration to methylborylethers, which upon hydrolysis can produce methanol. These organocatalysts feature carbon-centered reversible CO2 binding, broad borane scopes, and high catalytic activities.
BICYCLIC AROMATIC CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
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Paragraph 0530; 0531, (2014/07/23)
The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
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Paragraph 0639; 0640, (2014/07/23)
The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
