74771-40-7Relevant academic research and scientific papers
Ligand-controlled Regiodivergent C?H Alkenylation of Pyrazoles and its Application to the Synthesis of Indazoles
Kim, Hyun Tae,Ha, Hyeri,Kang, Geunhee,Kim, Og Soon,Ryu, Ho,Biswas, Abul Kalam,Lim, Sang Min,Baik, Mu-Hyun,Joo, Jung Min
, p. 16262 - 16266 (2017)
Regioselective C4-, C5-, and di-alkenylations of pyrazoles were achieved. An electrophilic Pd catalyst generated by trifluoroacetic acid (TFA) and 4,5-diazafluoren-9-one (DAF) leads to C4-alkenylation, whereas KOAc and mono-protected amino acid (MPAA) ligand Ac-Val-OH give C5-alkenylation. A combination of palladium acetate, silver carbonate, and pivalic acid affords dialkenylation products. Annulation through sequential alkenylation, thermal 6π-electrocyclization, and oxidation gives functionalized indazoles. This comprehensive strategy greatly expands the range of readily accessible pyrazole and indazole derivatives, enabling useful regiodivergent C?H functionalization of pyrazoles and other heteroaromatic systems.
MTA-Cooperative PRMT5 Inhibitors
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Paragraph 0298, (2021/03/19)
The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
Method for synthesizing trans-olefin compound
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Paragraph 0099-0102, (2020/06/20)
The invention discloses a trans-olefin compound synthesis method, which comprises: carrying out a heating reaction on an alkyne compound represented by a general formula (I), a reducing agent and a solvent to obtain a trans-olefin compound represented by a general formula (II), wherein the synthesis route is as follows: R1 and R2 are independently selected from hydrogen, alkyl, cycloalkyl or aryl;wherein the reducing agent is a sulfur-containing compound and is selected from at least one of thioacetamide, N,N-dimethyl dithiocarbamate dimethyl ammonium salt, dimethyl amino sodium dithioformatedihydrate, potassium ethyl xanthate and potassium isopropyl xanthate. According to the method, a cheap, efficient and safe reducing agent is utilized to realize high-selectivity reduction of alkyne to prepare trans-olefin under the condition of no transition metal catalysis, so that the method is simple and easy to implement, wide in substrate application range and easy to realize industrialization.
Xanthate-mediated synthesis of (E)-alkenes by semi-hydrogenation of alkynes using water as the hydrogen donor
Luo, Xianglin,Chen, Xiuwen,Chen, Lu,Zhang, Kun,Li, Yibiao
supporting information, p. 2170 - 2173 (2019/02/24)
Semi-hydrogenation of alkynes is one of the most widely used methods for obtaining alkenes in laboratory preparation and in industry. Transition metal catalysts have been extensively studied for this transformation, but the tolerance of functional groups, such as pyridine,-OH,-NH2,-Bpin, and halides, and the toxicity of the trace amount of transition metal catalysts are still highly challenging. In this study, we report a general and robust strategy to achieve the semi-hydrogenation of alkynes using inexpensive and commercially available xanthate as the mediator. Mechanism studies support a non-radical process and H2O acts as the hydrogen donor.
ETHINYL-PYRAZOLE DERIVATIVE
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Paragraph 0219; 0220, (2013/05/22)
Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof i
HETEROARYL-PYRAZOLE DERIVATIVE
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Paragraph 0267; 0268, (2013/06/05)
A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.
THERMAL DECOMPOSITION OF 1,2-DIMETHYL-3(5)-(4-R-STYRYL)PYRAZOLIUM IODIDES
Perevalov, V. P.,Andreeva, M. A.,Shmelev, L. V.,Stepanov, B. I.
, p. 1266 - 1269 (2007/10/02)
The reaction of 1,2,3,(5)-trimethylpyrazolium iodide with aromatic aldehydes yielded the series of 1,2-dimethyl-3(5)-(4-R-styryl)pyrazolium iodides (R = H, NMe2, NO2).The quantitative ratio of 1-methyl-3- and -5-(4-R-styryl)pyrazoles formed in the thermal decomposition of the above-mentioned pyrazolium iodides depends on steric factors in the initial compounds and on the electronic influence of the substituent R.A simple method was proposed for the production of trans,trans-1,4-bis(1-methyl-3-pyrazolylvinyl)benzene and 1-methyl-3,5-distyrylpyrazole, which possess fluorescent properties.
