2167-14-8Relevant articles and documents
Effect of aromatic π-bridges on molecular structures and optoelectronic properties of A-π-D-π-A small molecular acceptors based on indacenodithiophene
Chen, Yueju,Liang, Jingtang,Shen, Ping,Wang, Linqiao,Weng, Chao,Yu, Yufu
, (2020/12/02)
Investigation on the relationship between molecular structure and device performance is of great important to develop highly efficient A-π-D-π-A small molecular acceptors (SMAs). However, there is still lack of a complete and in-depth study on effects of
Preparation method for N-ethyl-2-aminomethylpyrrolidine
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, (2018/05/16)
The invention relates to a preparation method for N-ethyl-2-aminomethylpyrrolidine. The preparation method comprises the following steps: with furfural as a raw material, subjecting the furfural to acetal protection so as to obtain furfural glycol acetal, allowing the furfural glycol acetal to react with ethylamine so as to generate 2-(1,3-dioxolan-2-yl)-N-ethylpyrrole, allowing the 2-(1,3-dioxolan-2-yl)-N-ethylpyrrole to react with diluted hydrochloric acid so as to generate N-ethylpyrrole-2-carbaldehyde, and subjecting the N-ethylpyrrole-2-carbaldehyde and liquid ammonia to palladium-carbonreductive ammoniation by one step so as to generate the N-ethyl-2-aminomethylpyrrolidine. The preparation method has a synthetic route which is described in the specification. The invention has the following advantages: the preparation method for the N-ethyl-2-aminomethylpyrrolidine provided by the invention starts with the furfural as a raw material to prepare a product through protection, amination and reductive ammoniation, and has the advantages of short reaction route, high yield capable of reaching 85% or above, little pollution and applicability to industrialization.
IMIDAZOLIDINONE DERIVATIVES AS INHIBITORS OF PERK
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Page/Page column 86, (2017/04/11)
The invention is directed to substituted imidazolidinone derivatives. Specifically, the invention is directed to compounds according to Formula I (I) wherein R1, R2, R3, R4, R5, R6, R7, X, Y1, Y2 and Z are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, pre-cancerous syndromes, as Alzheimer's disease, neuropathic pain, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, Parkinson disease, diabetes, metabolic syndrome, metabolic disorders, Huntington's disease, Creutzfeldt-Jakob Disease, fatal familial insomnia, Gerstmann-Str?ussler-Scheinker syndrome, and related prion diseases, amyotrophic lateral sclerosis, progressive supranuclear palsy, myocardial infarction, cardiovascular disease, inflammation, organ fibrosis, chronic and acute diseases of the liver, fatty liver disease, liver steatosis, liver fibrosis, chronic and acute diseases of the lung, lung fibrosis, chronic and acute diseases of the kidney, kidney fibrosis, chronic traumatic encephalopathy (CTE), neurodegeneration, dementias, frontotemporal dementias, tauopathies, Pick's disease, Neimann-Pick's disease, amyloidosis, cognitive impairment, atherosclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Pyrrolic molecular rotors acting as viscosity sensors with high fluorescence contrast
Lee, Seung-Chul,Heo, Jeongyun,Ryu, Jong-Wan,Lee, Chang-Lyoul,Kim, Sehoon,Tae, Joon-Sung,Rhee, Byung-Ohk,Kim, Sang-Wook,Kwon, O-Pil
supporting information, p. 13695 - 13698 (2016/11/29)
New pyrrolic viscosity sensors exhibit one order of magnitude higher fluorescence contrast compared to that of the conventional phenolic analogues due to the viscosity-sensitive rotation of the asymmetric pyrrole group and successfully demonstrate mapping
ANTI-FIBROTIC PYRIDINONES
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Paragraph 0627, (2015/11/02)
This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.
ANTI-FIBROTIC PYRIDINONES
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Paragraph 0838-0839, (2014/04/17)
Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
SPIRO AZETIDINE ISOXAZOLE DERIVATIVES AND THEIR USE AS SSTR5 ANTAGONISTS
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Paragraph 0409, (2014/09/29)
Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification.
Flash vacuum pyrolysis of 2,2-dioxo-1H,3H-pyrrolo[1,2-c]thiazoles and 2-vinyl-1H-pyrroles
Soares, Maria I.L.,Lopes, Susana M.M.,Cruz, Pedro F.,Brito, Rui M.M.,Pinho e Melo, Teresa M.V.D.
, p. 9745 - 9753 (2008/12/22)
The flash vacuum pyrolysis of new 1,1-dimethyl- and 1-methyl-1H,3H-pyrrolo[1,2-c]thiazole-2,2-dioxides gave penta-substituted 2-vinyl-1H-pyrroles via sigmatropic [1,8]-H shift of the corresponding azafulvenium methide intermediates. In some cases these 1H-pyrroles underwent rearrangement to 2-allyl-1H-pyrroles. Di-substituted 2-vinylpyrroles have also been prepared and their reactivity studied. Under FVP N-benzyl-pyrrol-2-ylpropenoates were converted into 3H-pyrrolizin-3-ones. On the other hand, microwave-assisted reaction of 1-benzyl-2-vinyl-1H-pyrrole gave a 4,5,6,7-tetrahydro-1H-indole derivative.
Acyl radical cyclisation onto pyrroles
Allin, Steven M.,Barton, William R.S.,Bowman,McInally, Tom
, p. 7887 - 7890 (2007/10/03)
Synthetically useful [1,2-a]-fused pyrroles, e.g. 2,3-dihydro-1H-pyrrolizidines substituted in the 1- and 7-positions, have been generated by acyl radical cyclisation onto pyrroles using N-(ω-acyl)-radicals generated from acyl-selenide precursors. The protocol does not require high pressures of CO. Mechanistic studies indicate the key role of azo radical initiators as oxidants of the intermediate π-radicals.
- and pyrroles as Thromboxane Synthetase Inhibitors
Martinez, Gregory R.,Walker, Keith A. M.,Hirschfeld, Donald R.,Maloney, Patrick J.,Yang, Diana S.,Rosenkranz, Roberto P.
, p. 890 - 897 (2007/10/02)
Several and pyrroles were prepared and evaluated in vitro as thromboxane synthetase inhibitors in human platelet aggregation studies.A number of structures, e.g. 10b,f,g,i (respective IC50 values: 1 μM, 50 nM, 42 nM, 44 nM) showed superior in vitro inhibition of TXA2 synthetase when compared to the standard dazoxiben (1).However, it was found that in vitro potency did not translate into nor correlate with in vivo activity when these compounds were evaluated in mice in a collagen-epinephrine-induced pulmonary thromboembolism model. (E)-1-Methyl-2--5-(2-carboxyprop-1-enyl)pyrrole (10b) was found to offer protection against collagen-epinephrine-induced mortality in mice, thereby demonstrating that oral administration is an effective route for absorption of this drug.Additional evidence for the oral effectiveness of 10b in lowering serum TXB2 levels was obtained by performing ex vivo radioimmunoassay experiments with rats.A 13-week study of 10b in rats with reduced renal mass was conducted in order to evaluate the role of TXA2 production in hypertension and renal dysfunction.Although serum and urinary TXB2 levels in rats were found to be lowered during this study by 10b, the levels of urinary protein excretion remained comparable to that of the control group.