61266-33-9Relevant academic research and scientific papers
Synthesis of Azepino[1,2-a]indole-10-amines via [6+1] Annulation of Ynenitriles with Reformatsky Reagent
Iioka, Ryoya,Yorozu, Kohei,Sakai, Yoko,Kawai, Rika,Hatae, Noriyuki,Takashima, Katsuki,Tanabe, Genzoh,Wasada, Hiroaki,Yoshimatsu, Mitsuhiro
, p. 1553 - 1558 (2021/02/26)
Lewis acid-catalyzed [6+1] annulation reactions of 2-cyano-1-propargyl- and 2-alkynyl-1-cyanomethyl-indoles with Reformatsky reagent are described. 8-Aryl, 8-alkyl-, 8-hetaryl-, 9-aryl, and 9-alkyl-azepino[1,2-a]indole amines were obtained through a 7-endo-mode cyclization of the β-aminoacrylate intermediates. The antiproliferative activity of the azepino[1,2-a]indoles analogs against the HCT-116 cells were also examined.
Transition-metal-free and facile synthesis of 3-alkynylpyrrole-2,4-dicarboxylates from methylene isocyanides and propiolaldehyde
Huo, Xiaoli,Chen, Xiaojuan,Yu, Liya,Zhang, Chong,Zeng, Linghui,Zhu, Huajian,Shao, Jiaan,Fu, Liping,Zhang, Jiankang
supporting information, p. 16430 - 16433 (2021/10/01)
A transition-metal-free, facile and efficient method for the synthesis of 3-alkynylpyrrole-2,4-dicarboxylates from methylene isocyanides and propiolaldehyde with moderate to good yields has been developed. The direct transformation process and good tolerance of various substituents make it an alternative approach to previous protocols, and potential applications of these investigated compounds are expected with or without post-modifications.
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Paragraph 00401; 00404; 00476; 00480, (2020/07/06)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
3-aryl-2-propyn-1-ol derivative and preparation method thereof
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Paragraph 0108-0120, (2020/12/31)
The invention discloses a 3-aryl-2-propyn-1-ol derivative and a preparation method thereof, belongs to the field of organic synthesis, and particularly relates to a 3-aryl-2-propyn-1-ol derivative anda preparation method thereof. A purpose of the invention is to solve the problems of high energy consumption, high cost and environmental pollution caused by conditions of high temperature, metal catalysis, strong base or low temperature and the like required by the synthesis of the existing 3-aryl-2-propyn-1-ol derivative. The structural formula of the 3-aryl-2-propyn-1-ol derivative is shown inthe specification. The method comprises the following steps: 1, sequentially adding an aryl acetylene compound, an ammonium salt, an alkali, water and an organic solvent into a three-necked flask, and electrolyzing at room temperature in an air atmosphere under a stirring condition; 2, extracting, and carrying out reduced pressure distillation to remove the solvent to obtain a crude product; and3, purifying the crude product through silica gel column chromatography to obtain the 3-aryl-2-propyn-1-ol derivative. According to the invention, the 3-aryl-2-propyn-1-ol derivative can be obtained.
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Paragraph 00230; 00527;00617, (2020/07/05)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
Cobalt-Catalyzed Asymmetric Hydroboration/Cyclization of 1,6-Enynes with Pinacolborane
Yu, Songjie,Wu, Caizhi,Ge, Shaozhong
supporting information, p. 6526 - 6529 (2017/05/29)
We report a cobalt-catalyzed asymmetric hydroboration/cyclization of 1,6-enynes with catalysts generated from Co(acac)2 and chiral bisphosphine ligands and activated in situ by reaction with pinacolborane (HBpin). A variety of oxygen-, nitrogen
Preparation of monoalkylpiperidines via the mild hydrogenation of monoalkynylpyridines
Usuki, Toyonobu,Komatsu, Akira
supporting information, p. 2856 - 2858 (2017/06/27)
Monoalkynylpyridines were prepared via a Sonogashira cross-coupling reaction between monoiodopyridines and alkynes. Mild hydrogenation of the obtained monoalkynylpyridines was then conducted to produce the corresponding monoalkylpiperidines in moderate to excellent yields. The hydrogenation reaction was carried out under H2 (1?atm) in the presence of 10?wt% Pd/C (5?eq) in either AcOH or MeOH at room temperature. The present mild method is therefore useful for the quick and easy preparation of monoalkylpiperidines.
METHOD FOR PRODUCING PIPERIDINE COMPOUND
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Paragraph 0057-0059, (2018/04/18)
PROBLEM TO BE SOLVED: To provide a method for producing a piperidine compound in an industrially convenient manner. SOLUTION: This invention relates to a method for producing a compound represented by general formula (I) or a salt thereof that includes the step of converting a pyridine compound having an alkynylene group in a side chain, by a contact hydrogenation reaction, into the compound represented by general formula (I) or a salt thereof (in the general formula (I), R1 is a hydrogen atom, a hydroxy group, or an optionally substituted alkyl group having carbon atoms of 1 or more and 20 or less). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
Chemoproteomics-Enabled Discovery of a Potent and Selective Inhibitor of the DNA Repair Protein MGMT
Wang, Chao,Abegg, Daniel,Hoch, Dominic G.,Adibekian, Alexander
supporting information, p. 2911 - 2915 (2016/02/27)
We present a novel chemical scaffold for cysteine-reactive covalent inhibitors. Chloromethyl triazoles (CMTs) are readily accessed in only two chemical steps, thus enabling the rapid optimization of the pharmacological properties of these inhibitors. We d
Pyrazine- and pyridine-substituted prop-2-yn-1-ols, but-3-yn-2-ols, and but-3-yn-2-ones –purification, stability, and handling revised
Schindler, Claudia,Schulzke, Carola
, p. 1008 - 1013 (2016/08/26)
A short series of alkynyl-substituted pyrazine and pyridine derivatives was synthesized by the palladium-catalyzed Sonogashira cross-coupling reactions between aryl halides and alkynes. All the products are either white solids or colorless liquids, which is partly in contrast to previous reports. After purification, a color change or intense darkening was observed, in some cases starting almost immediately. Both, the nature of the heteroaromatic ring and the substituents of the alkyne moiety affect their stability. Herein details of synthesis, characterization, and, most importantly, purification and handling are reported.
