15118-67-9Relevant articles and documents
Synthesis of Unsymmetrical 1,4-Dicarbonyl Compounds by Photocatalytic Oxidative Radical Additions
Dong, Ya,Li, Ruining,Zhou, Junliang,Sun, Zhankui
, p. 6387 - 6390 (2021/08/23)
Herein we report a photocatalytic oxidative radical addition reaction for the synthesis of unsymmetrical 1,4-dicarbonyl compounds. This reaction utilizes a desulfurization process to generate electrophilic radicals, which add to α-halogenated alkenes and undergo further oxidation to deliver 1,4-dicarbonyl compounds. This mild and highly efficient method provides a valuable alternative to known strategies.
Combined Photoredox/Enzymatic C?H Benzylic Hydroxylations
Betori, Rick C.,May, Catherine M.,Scheidt, Karl A.
supporting information, p. 16490 - 16494 (2019/11/03)
Chemical transformations that install heteroatoms into C?H bonds are of significant interest because they streamline the construction of value-added small molecules. Direct C?H oxyfunctionalization, or the one step conversion of a C?H bond to a C?O bond, could be a highly enabling transformation due to the prevalence of the resulting enantioenriched alcohols in pharmaceuticals and natural products,. Here we report a single-flask photoredox/enzymatic process for direct C?H hydroxylation that proceeds with broad reactivity, chemoselectivity and enantioselectivity. This unified strategy advances general photoredox and enzymatic catalysis synergy and enables chemoenzymatic processes for powerful and selective oxidative transformations.
A process for preparing γ - ketone carbonyl compounds
-
Paragraph 0106; 0107; 0108, (2018/07/30)
The present invention discloses a gamma-ketone carbonyl compound preparation method, wherein in the presence of an oxidizing agent, a styrene compound and ethyl diazoacetate are adopted as reactants, copper or a copper compound is adopted as a catalyst, DABCO is adopted as an alkali, and a free radical reaction is performed in a polar solvent isopropyl alcohol to obtain the product gamma-ketone carbonyl compound. According to the method of the present invention, the reaction activity of the catalyst is high, the reaction conditions are mild, the substrate application range is wide, the post-treatment is convenient, the yield of the target product is high, the preparation process is simple, and the sources of the used raw materials are wide.
Discovery of Oxime Ethers as Hepatitis B Virus (HBV) Inhibitors by Docking, Screening and In Vitro Investigation
Tan, Jie,Zhou, Min,Cui, Xinhua,Wei, Zhuocai,Wei, Wanxing
, (2018/03/29)
A series of oxime ethers with C6-C4 fragment was designed and virtually bioactively screened by docking with a target, then provided by a Friedel-Crafts reaction, esterification (or amidation), and oximation from p-substituted phenyl derivatives (Methylbenzene, Methoxybenzene, Chlorobenzene). Anti-hepatitis B virus (HBV) activities of all synthesized compounds were evaluated with HepG2.2.15 cells in vitro. Results showed that most of compounds exhibited low cytotoxicity on HepG2.2.15 cells and significant inhibition on the secretion of HBsAg and HBeAg. Among them, compound 5c-1 showed the most potent activity on inhibiting HBsAg secretion (IC50 = 39.93 μM, SI = 28.51). Results of the bioactive screening showed that stronger the compounds bound to target human leukocyte antigen A protein in docking, the more active they were in anti-HBV activities in vitro.
Useful thiophene derivatives in the treatment of diabetes
-
Page/Page column 89, (2017/10/24)
The present invention relates to a thiophene derivative of the following general formula I or an enantiomer, diastereoisomer, hydrate, solvate, tautomer, racemic mixture or pharmaceutically acceptable salt thereof or to its use as a drug in particular intended for treating and/or preventing diabetes, its complications and/or associated pathologies, advantageously diabetes of type II and hyperglycemia.
Phenyl substituted pyridazine structure unit containing compounds and methods for their preparation and use
-
Paragraph 0085-0086; 0135-0136, (2016/11/17)
The invention discloses compounds containing phenyl substituted pyridazine structural unit, and a preparation method and application thereof. The structural general formula of the compounds containing phenyl substituted pyridazine structural unit is disclosed as Formula I. The compounds disclosed as Formula I have proper nuclear magnetic detection; and in order to solve the problems of less research on near-infrared materials and deficiency in high-efficiency high-stability near-infrared luminescent materials at present stage, the invention provides a series of near-infrared luminescent materials containing phenyl substituted pyridazine structure. The compounds have the advantages of accessible raw material, simple preparation process and high overall yield, and have important application value for researching development and application of near-infrared materials.
Cu-based carbene involved in a radical process: A new crossover reaction to construct γ-peroxy esters and 1,4-dicarbonyl compounds
Jiang, Jiewen,Liu, Jiajun,Yang, Ling,Shao, Ying,Cheng, Jiang,Bao, Xiaoguang,Wan, Xiaobing
supporting information, p. 14728 - 14731 (2015/10/05)
Through merging Cu-based carbenes in a radical process, a novel crossover reaction has been successfully established, leading to the facile and efficient syntheses of various γ-peroxy esters and 1,4-dicarbonyl compounds. Considering that both Cu-based carbene complexes and radicals are extremely reactive, and therefore exist only in extraordinarily low concentrations, the high selectivity of this coupling reaction is unusual.
USEFUL THIOPHENE DERIVATIVES IN THE TREATMENT OF DIABETES
-
Paragraph 0137, (2015/07/22)
The present invention relates to a thiophene derivative of the following general formula I or an enantiomer, diastereoisomer, hydrate, solvate, tautomer, racemic mixture or pharmaceutically acceptable salt thereof or to its use as a drug in particular intended for treating and/or preventing diabetes, its complications and/or associated pathologies, advantageously diabetes of type II and hyperglycemia.
Efficient hydroxymethylation reactions of iodoarenes using CO and 1,3-dimethylimidazol-2-ylidene borane
Kawamoto, Takuji,Okada, Takuma,Curran, Dennis P.,Ryu, Ilhyong
supporting information, p. 2144 - 2147 (2013/06/05)
A hydroxymethylation reaction of a variety of iodoarenes proceeded effectively in the presence of CO, NHC-borane, diMeImd-BH3 (2) as a radical mediator, and a catalytic amount of AIBN. The reaction took place chemoselectively at the aryl-iodine bond but not at the aryl-bromine and aryl-chlorine bonds. A three-component coupling reaction comprising aryl iodides, CO, and electron-deficient alkenes also proceeded well to give unsymmetrical ketones in good yields. Control experiments show that 2 would act as a hydrogen donor to acyl radicals and iodinated NHC-borane as a reducing agent of aldehydes.
Tris(4-methoxylphenyl)phosphine-catalyzed C-C bond formation reaction: Mutual addition of aromatic aldehydes and ethyl acrylate
Teng, Jun-Jiang,Qiao, Yan-Hui,Zhang, Qing,Li, Chun-Hai,Huang, Min
, p. 848 - 858 (2013/02/25)
A highly efficient intermolecular mutual addition of aromatic aldehydes with ethyl acrylate was developed by using tris(4-methoxylphenyl)phosphine as the catalyst. The reaction corresponds to the construction of 1,4-dicarbonyl compound and allylic alcohol
