27631-29-4Relevant articles and documents
2,4- Dichloro -6,7-dimethoxyquinazoline solvate and preparation method thereof (by machine translation)
-
Paragraph 0039-0041, (2020/06/02)
The invention provides 2,4 - dichloro - 66667-dimethoxyquinazoline solvate, and the solvate has the chemical structure: shown in the formula I. A specific preparation method is: dichloro - 666627-dimethoxyquinazoline solvate 2,4 - obtained by adding first kinds of solvent, stirring crystallization; to the quinazoline concentrate second of - 5 5 5 5 5-dimethoxyquinazoline solvate by stirring, through filtration, drying, to obtain a pale yellow crystalline solid powder, which is a, dichloro - 666627-dimethoxyquinazolinazolinazolinazolinazolinone chemical unstable. 2,4 - 2,4 - in drying and, storage. The present invention relates to a method for preparing the intermediate 2,4 - in a dry state. (by machine translation)
Combining Isocyanides with Carbon Dioxide in Palladium-Catalyzed Heterocycle Synthesis: N3-Substituted Quinazoline-2,4(1H,3H)-diones via a Three-Component Reaction
Mampuys, Pieter,Neumann, Helfried,Sergeyev, Sergey,Orru, Romano V. A.,Jiao, Haijun,Spannenberg, Anke,Maes, Bert U. W.,Beller, Matthias
, p. 5549 - 5556 (2017/08/17)
We report a Pd-catalyzed three-component reaction of 2-bromoanilines, carbon dioxide, and isocyanides. The combination of these two readily available C1-reactants, featuring a huge difference in kinetic and thermodynamic stability, is hitherto unprecedented in transition-metal catalysis. With this one-pot three-component reaction, N3-substituted quinazoline-2,4(1H,3H)-diones are obtained in moderate to high yields in a completely regio- and chemoselective manner. Our approach easily allows variation of the arene and N3-substitution pattern of the desired heterocycle. The formal synthesis of different APIs illustrates its practical applicability. In addition, the methodology also allows for a convenient and selective 13C-labeling through the use of 13CO2. This is illustrated for [2-13C]-2,4-dichloro-6,7-dimethoxyquinazoline synthesis, a key intermediate for several APIs.
Function-oriented development of CXCR4 antagonists as selective human immunodeficiency virus (HIV)-1 entry inhibitors
Wu, Chien-Huang,Wang, Chuan-Jen,Chang, Chun-Ping,Cheng, Yung-Chi,Song, Jen-Shin,Jan, Jiing-Jyh,Chou, Ming-Chen,Ke, Yi-Yu,Ma, Jing,Wong, Ying-Chieh,Hsieh, Tsung-Chih,Tien, Yun-Chen,Gullen, Elizabeth A.,Lo, Chen-Fu,Cheng, Chia-Yi,Liu, Yu-Wei,Sadani, Amit A.,Tsai, Chia-Hua,Hsieh, Hsin-Pang,Tsou, Lun K.,Shia, Kak-Shan
, p. 1452 - 1465 (2015/03/04)
Motivated by the pivotal role of CXCR4 as an HIV entry co-receptor, we herein report a de novo hit-to-lead effort on the identification of subnanomolar purine-based CXCR4 antagonists against HIV-1 infection. Compound 24, with an EC50 of 0.5 nM against HIV-1 entry into host cells and an IC50 of 16.4 nM for inhibition of radioligand stromal-derived factor-1α (SDF-1α) binding to CXCR4, was also found to be highly selective against closely related chemokine receptors. We rationalized that compound 24 complementarily interacted with the critical CXCR4 residues that are essential for binding to HIV-1 gp120 V3 loop and subsequent viral entry. Compound 24 showed a 130-fold increase in anti-HIV activity compared to that of the marketed CXCR4 antagonist, AMD3100 (Plerixafor), whereas both compounds exhibited similar potency in mobilization of CXCR4+/CD34+ stem cells at a high dose. Our study offers insight into the design of anti-HIV therapeutics devoid of major interference with SDF-1α function.
