3080-99-7Relevant academic research and scientific papers
REACTION BETWEEN N-ACYL-2,3-DIHYDROBENZO-1,4-THIAZINE AND N-ACYLPHENOTIAZINE WITH ORGANOMETALLIC REAGENTS
Ciminale, Francesco,Dunno, Leonardo Di,Florio, Saverio
, p. 3001 - 3002 (1980)
The title N-acyl-derivatives react with n-BuLi and Grignard reagents leading to products, which, formally, can be considered as derived from a Claisen-type condensation reaction.
Influenza virus replication inhibitors and uses thereof
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Paragraph 0269-0273, (2021/07/01)
The invention belongs to the field of medicines, and particularly relates to novel compounds serving as an influenza virus replication inhibitor, a preparation method thereof, a pharmaceutical composition containing the compounds and application of the compounds and the pharmaceutical composition in treatment of influenza. The compounds are compounds as shown in a formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrugs of the stereoisomer, the tautomer, the nitrogen oxide, the solvate, the metabolite and the pharmaceutically acceptable salt of the compound as shown in the formula (I). The compounds not only can well inhibit influenza viruses, but also have lower cytotoxicity, excellent in-vivo pharmacokinetic property and the in-vivo pharmacodynamic property and good liver microsome stability.
Design, Synthesis, Safener Activity, and Molecular Docking of Novel N-Substituted Thiazide/Thiazole Derivatives
Fu, Ying,Yi, Ke-Han,Li, Ming-Qiang,Wang, Jing-Yi,Chen, Yu-Feng,Ye, Fei
, p. 180 - 187 (2018/11/25)
A series of novel substituted thiazide/thiazole compounds were designed by splicing active groups and bioisosterism. The title compounds were synthesized via the cyclization, acylation, and carbamylation. All the compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS. The single crystal of compound 3f was determined by X-ray crystallography. The biological activity tests indicated that all the compounds showed potential safener activity to the herbicide chlorsulfuron, in which compound 3e showed almost the same level as the commercialized safener AD-67. The molecular docking results were in good agreement with the bioassay results, which demonstrated that compound 3e might compete with chlorsulfuron in the acetolactate synthase active site, causing the herbicide ineffective in maize.
Sodium Triethylborohydride-Catalyzed Controlled Reduction of Unactivated Amides to Secondary or Tertiary Amines
Yao, Wubing,He, Lili,Han, Deman,Zhong, Aiguo
, (2019/11/14)
The first transition-metal-free catalytic protocol for controlled reduction of amide functions using cheap and bench-stable hydrosilanes as reducing agents has been established. By altering the hydrosilane and solvent, the new method enables the selective cleavage of unactivated C-O bonds in amides and allows the C-N bonds to selectively break via the deacylated cleavage. Overall, this novel process may offer a versatile alternative to current methodologies employing stoichiometric metal systems for the controlled reduction of carboxamides.
Sodium Triethylborohydride-Catalyzed Controlled Reduction of Unactivated Amides to Secondary or Tertiary Amines
Yao, Wubing,He, Lili,Han, Deman,Zhong, Aiguo
, p. 14627 - 14635 (2019/12/02)
The first transition-metal-free catalytic protocol for controlled reduction of amide functions using cheap and bench-stable hydrosilanes as reducing agents has been established. By altering the hydrosilane and solvent, the new method enables the selective cleavage of unactivated C-O bonds in amides and allows the C-N bonds to selectively break via the deacylated cleavage. Overall, this novel process may offer a versatile alternative to current methodologies employing stoichiometric metal systems for the controlled reduction of carboxamides.
TETRAHYDROQUINOLINE SUBSTITUTED HYDROXAMIC ACIDS AS SELECTIVE HISTONE DEACETYLASE 6 INHIBITORS
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Paragraph 0231-0232, (2017/09/08)
Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, tr
Novel nonmetal catalytic bidirectional selective reduction method of tertiary aromatic amide
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Paragraph 0106; 0107; 0108; 0109, (2017/10/22)
The invention relates to a novel effective bidirectional selective environment-friendly method for hydrosilation reduction of tertiary aromatic amide and an organic silicon reagent. The method comprises the following steps: selecting a nonmetal catalytic system, and selectively preparing a secondary or tertiary organic amine compound by successively catalyzing tertiary aromatic amide and cheap PHMS or triethoxysilane under a mild condition. By adopting the method, the bidirectional selective reduction of the tertiary aromatic amide is realized by innovatively utilizing an electronic effect and steric hindrance difference of an organic silicon reagent at first time, so that a brand new strategy is provided for the reduction of amide and derivative of the amide, the defects of the traditional method that the substrate functional group is poor in compatibility, the production cost is high and the like can be overcome, and the application prospect of the amine compound prepared in industrial production or laboratory is promising.
Chemoselective Deprotection of Sulfonamides under Acidic Conditions: Scope, Sulfonyl Group Migration, and Synthetic Applications
Javorskis, Tomas,Orentas, Edvinas
, p. 13423 - 13439 (2017/12/26)
Chemoselective acidic hydrolysis of sulfonamides with trifluoromethanesulfonic acid has been evaluated as a deprotection method and further extended to more complex synthetic applications. In contrast to conventional troublesome sulfonamide hydrolysis, a near-stoichiometric amount of acid was found to be sufficient to bring about efficient deprotection of various neutral or electron-deficient N-arylsulfonamides, whereas electron-rich substrates provided sulfonyl group migration products. The deprotection method developed is fully selective for N-arylsulfonamides, and the possibility to discriminate among various different sulfonamides is demonstrated.
TRICYCLIC INDOLE MCL-1 INHIBITORS AND USES THEREOF
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Paragraph 0427, (2016/05/19)
The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.
An odorless, one-pot synthesis of nitroaryl thioethers via SNAr reactions through the in situ generation of S-alkylisothiouronium salts
Lu, Guo-Ping,Cai, Chun
, p. 59990 - 59996 (2015/02/19)
A newly developed C-S bond formation nucleophilic aromatic substitution (SNAr) reaction in aqueous Triton X-100 (TX100) micelles has been disclosed. This chemistry, in which odorless, cheap and stable thiourea in place of thiols is used as the sulfur reagent, provides an efficient approach for the generation of nitroaryl thioethers, which are useful structural units of many bioactive molecules, rendering this methodology attractive to both synthetic and medicinal chemistry.
