124623-15-0Relevant articles and documents
Design of new reaction conditions for the Sugasawa reaction based on mechanistic insights
Prasad, Kapa,Lee, George T.,Chaudhary, Apurva,Girgis, Michael J.,Streemke, James W.,Repic, Oljan
, p. 723 - 732 (2003)
A process to prepare 2-propionyl-4-bromoaniline by ortho acylation of 4-bromoaniline under Sugasawa conditions was developed. Upon scale-up in a pilot plant, the process gave lower yields than in the laboratory in four out of five plant runs. Analysis of
1,2,4-TRIAZINE-3-AMINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF IN MEDICINE
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Paragraph 0287; 0288, (2019/11/28)
The present invention relates to a 1,2,4-triazine-3-amine derivative, a preparation therefor, and use thereof in medicine. Specifically, the present invention relates to a 1,2,4-triazine-3-amine derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and use thereof as a therapeutic agent, in particular as an A2a receptor antagonist, and use thereof in the preparation of a medicament for treating a condition or disorder that is ameliorated by means of inhibition of the A2a receptor, each substituent in general formula (I) being same as defined in the description.
Catalyst-free geminal aminofluorination of ortho-sulfonamide-tethered alkylidenecyclopropanes via a Wagner-Meerwein rearrangement
Fan, Xing,Wang, Qiang,Wei, Yin,Shi, Min
supporting information, p. 10503 - 10506 (2018/09/21)
A catalyst-free intramolecular geminal aminofluorination of ortho-sulfonamide-tethered alkylidenecyclopropanes has been developed. The reaction proceeded through two SET processes with Selectfluor to give a fluorinated cyclopropylcarbinyl cation and a further Wagner-Meerwein rearrangement to generate a cyclobutyl carbocation, which undergoes intramolecular nucleophilic capture by amide to forge fluorinated cyclobuta[b]indoline derivatives. A polycyclic multi-fluorinated byproduct was also formed through a Ritter-type reaction in some cases.
QUINAZOLINE-BASED KINASE INHIBITORS
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Page/Page column 71, (2016/04/26)
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5′-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators
Kern, Jeffrey C.,Terefenko, Eugene A.,Fensome, Andrew,Unwalla, Ray,Wrobel, Jay,Cohen, Jeffrey,Zhu, Yuan,Berrodin, Thomas J.,Yudt, Matthew R.,Winneker, Richard C.,Zhang, Zhiming,Zhang, Puwen
scheme or table, p. 5015 - 5017 (2009/05/30)
A series of novel 7-(5′-cyanopyrrol-2-yl) substituted benzo[1,4]oxazepin-2-ones were prepared and tested for their progesterone receptor (PR) agonist or antagonist activity in the alkaline phosphatase assay using the human T47D breast carcinoma cell line.
Synthesis and antitumor activity of 20(S)-camptothecin derivatives. A-ring-substituted 7-ethylcamptothecins and their E-ring-modified water-soluble derivatives
Yaegashi,Sawada,Nagata,Furuta,Yokokura,Miyasaka
, p. 2518 - 2525 (2007/10/02)
Twenty-six novel A-ring-modified 7-ethylcamptothecins (6) were synthesized by Friedlander's condensation of the chiral tricyclic ketone (5) with aminopropiophenones (4). The compounds substituted with fluorine at the 11 position showed strong cytotoxicity
Camptothecin derivatives
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, (2008/06/13)
New campotothecin derivatives and a process for preparing same are disclosed, which are represented by the general formula: STR1 wherein R1 represents a lower alkyl group, R2 represents a hydrogen atom or an amino, hydroxyl, lower acylamino or lower alkoxy group, R3 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, nitro, amino, cyano or di(lower alkyl)amino group, R4 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, lower alkylthio, amino, cyano or di(lower alkyl)amino group, and R5 represents a hydrogen or halogen atom or a hydroxyl or lower alkoxy group, with the proviso that all of the R2, R3, R4 and R5 substituents should not be a hydrogen atom and also that if any one of the R2, R3, R4 and R5 is a hydroxyl or lower alkoxy group, all of the other three substituents should not be a hydrogen atom.