21900-40-3Relevant academic research and scientific papers
Improved synthesis of sterically encumbered heteroaromatic biaryls from aromatic β-keto esters
Rosen, Brandon R.,Ul Sharif, Ehesan,Miles, Dillon H.,Chan, Nicholas S.,Leleti, Manmohan R.,Powers, Jay P.
supporting information, (2020/03/25)
A protocol for the synthesis of hindered 4-aryl 2-aminopyrimidines from β–keto esters is described. The process employs trifluoroethanol as an essential additive to promote the guanidine condensation reaction, enabling the synthesis of 25 aryl- and heteroaryl substituted aminopyrimidines in good yields and high purities with no column chromatography. The conditions described herein are readily scalable and have been employed in the large-scale synthesis of the clinical A2a/A2bR antagonist AB928.
N-Heterocyclic Carbene Catalyzed Photoenolization/Diels–Alder Reaction of Acid Fluorides
Agrawal, Arush,G?tze, Jan P.,Golz, Paul,Hopkinson, Matthew N.,Mavroskoufis, Andreas,Rajes, Keerthana,Ru?, Vincent
supporting information, p. 3190 - 3194 (2020/01/24)
The combination of light activation and N-heterocyclic carbene (NHC) organocatalysis has enabled the use of acid fluorides as substrates in a UVA-light-mediated photochemical transformation previously observed only with aromatic aldehydes and ketones. Stoichiometric studies and TD-DFT calculations support a mechanism involving the photoactivation of an ortho-toluoyl azolium intermediate, which exhibits “ketone-like” photochemical reactivity under UVA irradiation. Using this photo-NHC catalysis approach, a novel photoenolization/Diels–Alder (PEDA) process was developed that leads to diverse isochroman-1-one derivatives.
Co(II)/Cu(II)-cocatalyzed oxidative C-H/N-H functionalization of benzamides with ketones: A facile route to isoindolin-1-ones
Zhou, Xi,Xu, Hongyan,Yang, Qiaodan,Chen, Hua,Wang, Shoufeng,Zhao, Huaiqing
supporting information, p. 8603 - 8606 (2019/07/25)
A cobalt and copper catalyzed reaction protocol has been developed to achieve the oxidative C-H/N-H annulation of benzamides containing an 8-aminoquinoline moiety as the directing group with ketones. Structurally diverse isoindolin-1-ones were furnished by the reaction of various substituent benzamides with ketones.
Synthesis and biological evaluation of 1,2,4-triazole-3-thione and 1,3,4-oxadiazole-2-thione as antimycobacterial agents
Sonawane, Amol D.,Rode, Navnath D.,Nawale, Laxman,Joshi, Rohini R.,Joshi, Ramesh A.,Likhite, Anjali P.,Sarkar, Dhiman
, p. 200 - 209 (2017/07/13)
Resistance among dormant mycobacteria leading to multidrug-resistant and extremely drug-resistant tuberculosis is one of the major threats. Hence, a series of 1,2,4-triazole-3-thione and 1,3,4-oxadiazole-2-thione derivatives (4a–5c) have been synthesized and screened for their antitubercular activity against Mycobacterium tuberculosis H37Ra (H37Ra). The triazolethiones 4b and 4v showed high antitubercular activity (both MIC and IC50) against the dormant H37Ra by in vitro and ex vivo. They were shown to have more specificity toward mycobacteria than other Gram-negative and Gram-positive pathogenic bacteria. The cytotoxicity was almost insignificant up to 100?μg/ml against THP-1, A549, and PANC-1 human cancer cell lines, and solubility was high in aqueous solution, indicating the potential of developing these compounds further as novel therapeutics against tuberculosis infection.
Silver-catalyzed oxidative activation of benzylic C-H bonds for the synthesis of difluoromethylated arenes
Xu, Peng,Guo, Shuo,Wang, Liyan,Tang, Pingping
supporting information, p. 5955 - 5958 (2014/06/10)
A mild and catalytic method to form difluoromethylated arenes through the activation of benzylic C-H bonds has been developed. Utilizing AgNO3 as the catalyst, various arenes with diverse functional groups undergo activation/fluorination of ben
IMIDAZOTRIAZINONE COMPOUNDS
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Paragraph 0543; 0544, (2013/10/08)
The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9 and pharmaceutically acceptable salt thereof. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including humans.
IMIDAZOTRIAZINONE COMPOUNDS
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Page/Page column 92-93, (2012/04/10)
The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including CNS or neurodegeneration disorder.
Process for Synthesizing Substituted Isoquinolines
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Page/Page column 5-6, (2010/04/23)
The present disclosure generally relates to a process for synthesizing optionally substituted 1-chloro-4-methoxyisoquinolines. The present disclosure also relates to intermediates useful in this process.
Hepatitis C Virus Inhibitors
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Page/Page column 35-36, (2009/12/02)
Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Hepatitis C Virus Inhibitors
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Page/Page column 15-16, (2009/12/05)
Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
