86-51-1Relevant academic research and scientific papers
V2O5@TiO2 Catalyzed Green and Selective Oxidation of Alcohols, Alkylbenzenes and Styrenes to Carbonyls
Upadhyay, Rahul,Kumar, Shashi,Maurya, Sushil K.
, p. 3594 - 3600 (2021/07/02)
The versatile application of different functional groups such as alcohols (1° and 2°), alkyl arenes, and (aryl)olefins to construct carbon-oxygen bond via oxidation is an area of intense research. Here, we report a reusable heterogeneous V2O5@TiO2 catalyzed selective oxidation of various functionalities utilizing different mild and eco-compatible oxidants under greener reaction conditions. The method was successfully applied for the alcohol oxidation, oxidative scission of styrenes, and benzylic C?H oxidation to their corresponding aldehydes and ketones. The utilization of mild and eco-friendly oxidizing reagents such as K2S2O8, H2O2 (30 % aq.), TBHP (70 % aq.), broad substrate scope, gram-scale synthesis, and catalyst recyclability are notable features of the developed protocol.
Palladium-Catalyzed Reductive Carbonylation of (Hetero) Aryl Halides and Triflates Using Cobalt Carbonyl as CO Source
Dogga, Bhushanarao,Joseph, Jayan T.,Kumar, C. S. Ananda
supporting information, p. 309 - 313 (2020/12/23)
An efficient protocol for the reductive carbonylation of (hetero) aryl halides and triflates under CO gas-free conditions using Pd/Co2(CO)8 and triethylsilane has been developed. The mild reaction conditions, enhanced chemoselectivity and, easy access to heterocyclic and vinyl carboxaldehydes highlights its importance in organic synthesis.
SUBSTITUTED-N-HETEROARYL COMPOUNDS AND USES THEREOF
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Page/Page column 76-77, (2020/01/24)
The present disclosure relates generally to compounds useful for the treatment and/or enhancement of cognitive function and negative symptoms associated with central nervous system disorders where the circuitry involving fast spiking PV+ interneurons and the production of cortical gamma oscillations is disrupted. The subject disclosure enables the manufacture of medicaments as well as compositions containing same for use in methods of therapy and prophylaxis of cognitive dysfunction and negative symptoms.
SUBSTITUTED-PYRIDINYL COMPOUNDS AND USES THEREOF
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Page/Page column 91, (2020/01/10)
The present application relates generally to compounds useful for the treatment and/or enhancement of cognitive dysfunction and negative symptoms associated with CNS disorders where the circuitry involving fast spiking PV+ interneurons and the production of cortical gamma oscillations is disrupted. The subject disclosure enables the manufacture of medicaments as well as compositions containing same for use in methods of therapy and prophylaxis of cognitive dysfunction and negative symptoms.
Method for fully synthesizing berberine
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, (2019/04/17)
The invention discloses a method for fully synthesizing berberine, and relates to a drug synthesis method. The method realizes the industrial full synthesis production of the berberine and is made from a bulk organic raw material catechol, the raw material is easily available, and the price is low; 2,3-dimethoxybenzaldehyde is obtained through selective formylation and methylation of the catechol;after a piperonyl ring is obtained through a catechol methylenenation reaction, piperonyl amine is synthesized through a one-step catalytic addition reaction, so that the synthesis steps of the piperonyl amine are shortened, the use of toxic cyanide is avoided, and the process is green and sustainable; condensation hydrogenation and salification reactions adopt a 'one-pot method', and thus the time and the energy are saved, and the cost is decreased. Industrialized full synthesis production of the berberine opens up large-scale production of the berberine, meets the clinical and research needs of the berberine in current anti-tumor, anti-blood pressure, anti-heart rhythm, blood sugar reduction, treatment of Alzheimer's disease and the like, provides effective drugs for reducing pain of patients, and has remarkable economic and social benefits.
Method for total synthesis of berberine with guaiacol as raw material
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, (2019/04/26)
The invention discloses a method for total synthesis of berberine with guaiacol as a raw material. According to a drug synthesis method, guaiacol serves as the raw material, 2-hydroxy-3-methoxybenzaldehyde is obtained through a selective formylation reaction, 2,3-dimethoxybenzaldehyde is obtained through a methylation reaction, pentamethyleneamine is obtained through a methylenenation reaction with catechol as a raw material, and homopiperony lamine is obtained through a one-step catalytic addition reaction; 2,3-dimethoxybenzaldehyde and homopiperony lamine are subjected to a one-pot condensation hydrogenation reaction under the condition of a nickel-based catalyst, hydrochloric acid is added to a reaction product, a crystal substance is cooled, after the reaction product is refined, hydrochloric acid is added, and cooling crystallization and filtration washing are conducted to obtain the product berberine. According to the method, the technology is simplified, and the use of toxic cyanide is avoided; 2,3-dimethoxybenzaldehyde and homopiperony lamine are subjected to a one-pot condensation hydrogenation and salifying technology, the time is saved, the energy is saved, and the costis lowered; in the technological process, solvents are recycled.
Highly Efficient Supramolecular Catalysis by Endowing the Reaction Intermediate with Adaptive Reactivity
Jiao, Yang,Tang, Bohan,Zhang, Yucheng,Xu, Jiang-Fei,Wang, Zhiqiang,Zhang, Xi
supporting information, p. 6077 - 6081 (2018/04/30)
A new strategy of highly efficient supramolecular catalysis is developed by endowing the reaction intermediate with adaptive reactivity. The supramolecular catalyst, prepared by host–guest complexation between 2,2,6,6-tetramethylpiperidin-1-oxyl (TEMPO) and cucurbit[7]uril (CB[7]), was used for biphasic oxidation of alcohols. Cationic TEMPO+, the key intermediate, was stabilized by the electrostatic effect of CB[7] in aqueous phase, thus promoting the formation of TEMPO+ and inhibiting side reactions. Moreover, through the migration into the organic phase, TEMPO+ was separated from CB[7] and recovered the high reactivity to drive a fast oxidation of substrates. The adaptive reactivity of TEMPO+ induced an integral optimization of the catalytic cycle and greatly improved the conversion of the reaction. This work highlights the unique advantages of dynamic noncovalent interactions on modulating the activity of reaction intermediates, which may open new horizons for supramolecular catalysis.
3-INDOLYL FURANOIDS AS INHIBITORS OF MATRIX METALLOPROTEINASE-9 FOR PREVENTION OF GASTRIC ULCER AND OTHER INFLAMMATORY DISEASES
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Paragraph 0082-0083, (2018/08/29)
Disclosed are 3-indolyl furanoid compounds which are useful as potent anti-inflammatory agents and prevent gastric ulcer by inhibiting matrix metalloproteinase-9 (MMP-9) expression in gastric mucosal layer. For example, disclosed is a compound of formula 1, wherein: R1 to R6 is selected from H, OH, CH3, OCH3, Br, Cl, Ph or o-OHC6H4, OCH2—CH═CH2, or OCH2CH2CH3, and R1 to R6 is having at least one substituent with alkyl, aryl and heteroaryl groups other than H, wherein the carbon in alkyl, aryl and heteroaryl is in the range of C1 to C8. Various embodiments relate to representative compounds of Formula 1 and method of preparation thereof. Further embodiments relates to the use of representative compounds of Formula 1 in treating diseases associated with gastric ulcer and other inflammatory diseases. A noted feature of an embodiment is the IC50 value of 50 μM of one of the 3-indolyl furanoids.
Design, synthesis and evaluation of curcumin-based fluorescent probes to detect Aβ fibrils
Sato, Taki,Hotsumi, Mayumi,Makabe, Koki,Konno, Hiroyuki
supporting information, p. 3520 - 3525 (2018/10/15)
Amyloid β fibrillation is an early event in Alzheimer's disease, so its detection is important to understand its roles in Alzheimer's disease. Curcumin, which has poor water solubility, has been reported to have many pharmacological activities including potent anti-amyloid β fibril activity in Alzheimer's disease. In this study, we found that curcumin analogues with the fluorescence property instead of non-inhibition of amyloid β fibrils. The development of new curcumin analogue, Me-CUR (9), as fluorescent switchable probe to detect amyloid β fibrils is described. Me-CUR (9) shows excellent fluorescence, especially higher than ThT (4), in the presence of amyloid β fibrils. These results suggest that Me-CUR (9) can become a useful in vitro amyloid fluorescence sensor for diagnosis of Alzheimer's disease.
Preparation method of 2,3-dimethoxybenzaldehyde
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Paragraph 0007-0010, (2018/12/03)
The invention discloses a preparation method of 2,3-dimethoxybenzaldehyde, and belongs to the technical field of medicine techniques. The technical problem to be solved by the invention relates to a more advanced preparation method of 2,3-dimethoxybenzaldehyde. The main point of the technical scheme for solving the technical problem by the invention is an innovative preparation method of the compound.
