42019-78-3Relevant articles and documents
Metal-free C-C bond formation: Via coupling of nitrile aimines and boronic acids
Livingstone, Keith,Bertrand, Sophie,Mowat, Jenna,Jamieson, Craig
, p. 10412 - 10416 (2019)
The challenges of developing sustainable methods of carbon-carbon bond formation remains a topic of considerable importance in synthetic chemistry. Capitalizing on the highly reactive nature of the nitrile imine 1,3-dipole, we have developed a novel metal-free coupling of this species with aryl boronic acids. Photochemical generation of a nitrile imine intermediate and trapping with a palette of boronic acids enabled rapid and facile access to a broad library of more than 25 hydrazone derivatives in up to 92% yield, forming a carbon-carbon bond in a metal free fashion. This represents the first reported example of direct reaction between boronic acids and a 1,3-dipole.
Selective Oxidation of Alkylarenes to the Aromatic Ketones or Benzaldehydes with Water
Du, Jihong,Duan, Baogen,Liu, Kun,Liu, Renhua,Yu, Feifei,Yuan, Yongkun,Zhang, Chenyang,Zhang, Jin
supporting information, (2022/02/09)
Here a palladium-catalyzed oxidation method for converting alkylarenes into the aromatic ketones or benzaldehydes with water as the only oxygen donor is reported. This C-H bond oxidation functionalization does not require other oxidants and hydrogen accep
Phenoxy aromatic acid compound with cyclopropyl and pharmaceutically acceptable salt thereof, and preparation method and application thereof
-
Paragraph 0040-0043, (2021/07/17)
The invention provides a phenoxy aromatic acid compound with cyclopropyl, a preparation method of the phenoxy aromatic acid compound, pharmaceutically acceptable salt of the phenoxy aromatic acid compound and a preparation method of the pharmaceutically acceptable salt of the phenoxy aromatic acid compound, and further provides dosage forms of the phenoxy aromatic acid compound and the pharmaceutically acceptable salt of the phenoxy aromatic acid compound and application of the phenoxy aromatic acid compound and the pharmaceutically acceptable salt of the phenoxy aromatic acid compound in drugs for treating hyperlipidemia diseases. The compound provided by the invention has a relatively good blood fat reducing drug effect, so that the compound has a very good application prospect.
Phenoxy aromatic acid with cyclopropyl and pharmaceutically acceptable salt thereof as well as preparation method and application thereof
-
Paragraph 0055-0057, (2021/07/17)
The invention provides phenoxy aromatic acid with cyclopropyl, a preparation method of the phenoxy aromatic acid, pharmaceutically acceptable salt of the phenoxy aromatic acid with cyclopropyl and a preparation method of the pharmaceutically acceptable salt, and further provides dosage forms of the phenoxy aromatic acid with cyclopropyl and the pharmaceutically acceptable salt of the phenoxy aromatic acid with cyclopropyl. The invention also discloses application of the compound in medicines for treating hyperlipidemia diseases. The compound provided by the invention has a relatively good blood fat reducing drug effect, so that the compound has a very good application prospect.
A sodium trifluoromethanesulfinate-mediated photocatalytic strategy for aerobic oxidation of alcohols
Zhu, Xianjin,Liu, Can,Liu, Yong,Yang, Haijun,Fu, Hua
supporting information, p. 12443 - 12446 (2020/10/30)
A sodium trifluoromethanesulfinate-mediated photocatalytic strategy for the aerobic oxidation of alcohols has been developed for the first time, and the photoredox aerobic oxidation of secondary and primary alcohols provided the corresponding ketones and carboxylic acids, respectively, in high to excellent yields.
Synthesis method of high-purity 4-chloro-4'-hydroxybenzophenone
-
Paragraph 0016-0030, (2020/01/25)
The invention relates to a synthesis method of high-purity 4-chloro-4'-hydroxybenzophenone. The method comprises the following steps: cooling chlorobenzene and anisole to 5 DEG C or below; adding anhydrous aluminum trichloride in three batches, controlling the temperature, dropwise adding a mixed solution of p-chlorobenzoyl chloride and chlorobenzene, and controlling the reaction temperature; maintaining the low temperature after addition is finished, raising the temperature to normal temperature, and maintaining the normal temperature for a reaction; adding anhydrous aluminum trichloride at atime, and then carrying out a two-stage heating reaction; performing cooling hydrolysis; and performing centrifuging, washing the crude product with a sodium carbonate solution and a sodium hydroxidesolution, adjusting the pH value with hydrochloric acid, and centrifugally separating out the refined product. The fine temperature control is combined with the control of the reaction time to reducebyproducts, so the purity reaches 99.9% or above.
Synthesis and evaluation of fenofibric acid ester derivatives: Studies of different formulation with their bioavailability and absorption conditions
Lv, Zhixiang,Wang, Zhou,Xiao, Fuyan,Jin, Guofan
, p. 280 - 287 (2020/01/03)
A series of fenofibric acid ester pro-drugs (JF-1-7) were synthesized. The pharmacokinetic properties of these pro-drugs were examined after oral administration to rats at a dose of 20 mg kg-1 to evaluate the relative bioavailability in rats. The bioavailability of the ester compounds, JF-1, 2, 3, 4, 5, 6, and 7, was significantly higher than that of fenofibrate. In particular, JF-2 proved to be most promising. The oral administration (20 mg kg-1) of JF-2 showed a relative bioavailability of approximately 272.8percent compared to fenofibrate.
Visible Light-Mediated [2 + 2] Cycloaddition Reactions of 1,4-Quinones and Terminal Alkynes
Sultan, Shaista,Bhat, Muneer-Ul-Shafi,Rizvi, Masood Ahmad,Shah, Bhahwal Ali
, p. 8948 - 8958 (2019/08/12)
A single-step synthesis of 4-hydroxy-functionalized bi-aryl and aryl/alkyl ketones via oxidative coupling of terminal alkynes with benzoquinones is reported. Furthermore, with naphthoquinones, owing to the cross-resonance of carbonyl with the aromatic ring, alkene-alkyne cycloaddition is more favored to give four-membered carbocyclic adducts, thereby precluding the requirement of preactivated alkynes.
Hydrogen bond directed aerobic oxidation of amines via photoredox catalysis
Wang, Hongyu,Man, Yunquan,Wang, Kaiye,Wan, Xiuyan,Tong, Lili,Li, Na,Tang, Bo
, p. 10989 - 10992 (2018/10/08)
An application of H-bonding interactions for directing the α-C-H oxidation of amines to amides and amino-ketones catalyzed by an organic photocatalyst is reported. The high efficiency of this method is demonstrated by the aerobic oxidation of pyrrolidines, diarylamines and benzylamines bearing urea groups with high yields and a wide substrate scope.
Preparation method of 4-chloro-4'-hydroxybenzophenone
-
Paragraph 0014; 0015; 0016, (2018/03/24)
The invention relates to a preparation method of 4-chloro-4'-hydroxybenzophenone. The preparation method comprises the following steps: adding a proper amount of dichloroethane, phenol, 4-chlorobenzonitrile, anhydrous zinc chloride and gel type strong-acid ion exchange resin into a reaction kettle and stirring; controlling temperature to 50 DEG C to 120 DEG C and continuously introducing dry hydrogen chloride gas until the 4-chlorobenzonitrile reacts completely; cooling to room temperature and adding a proper amount of a hydrochloric acid solution; raising the temperature, reflowing and reacting for 5h to 7h; then cooling to room temperature and layering; recycling the dichloroethane into an organic layer and adding alkali into residues and dissolving; de-coloring by utilizing active carbon, carrying out acid precipitation, extracting and filtering and drying to obtain the 4-chloro-4'-hydroxybenzophenone. The preparation method of the 4-chloro-4'-hydroxybenzophenone, provided by the invention, is simple in route and high in yield.