33844-23-4Relevant academic research and scientific papers
QUINAZOLINE DERIVATIVES AS PDE10A ENZYME INHIBITORS
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Page/Page column 51; 52, (2013/04/24)
This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The pr
Trifluoromethyl-promoted homocamptothecins: Synthesis and biological activity
Zhu, Lingjian,Miao, Zhenyuan,Sheng, Chunquan,Guo, Wei,Yao, Jianzhong,Liu, Wenfeng,Che, Xiaoying,Wang, Wenya,Cheng, Pengfei,Zhang, Wannian
experimental part, p. 2726 - 2732 (2010/08/07)
The homocamptothecin (hCPT) represents a new class of topoisomerase inhibitor which combines enhanced plasma stability and strong antitumor activity. Fluorine imparts desirable characteristics to drugs by modulating both the pharmacokinetics and pharmacodynamic properties of a drug. Therefore, in an attempt to improve the antitumor activity of homocamptothecins, seven new 7-trifluoromethylated homocamptothecin derivatives were prepared by proline-catalyzed Friedlander annulation. The antitumor activity in vitro and in vivo on cancer cell lines, and inhibitory properties of topoisomerase I-mediated DNA cleavage of compounds 6c and 8b were evaluated. Several of these trifluoromethylated hCPT derivatives (such as 6a, 6b and 6c) possessed higher in vitro antitumor activity than topotecan (TPT). Especially, the compound 6c showed effective in vivo antitumor activity comparable to that of TPT.
Practical synthesis of 2-(2-isopropylaminothiazol-4-yl)-7-methoxy-1H- quinolin-4-one: Key intermediate for the synthesis of potent HCV NS3 protease inhibitor BILN 2061
Frutos, Rogelio P.,Haddad, Nizar,Houpis, Ioannis N.,Johnson, Michael,Smith-Keenan, Lana L.,Fuchs, Victor,Yee, Nathan K.,Farina, Vittorio,Faucher, Anne-Marie,Brochu, Christian,Hache, Bruno,Duceppe, Jean-Simon,Beaulieu, Pierre
, p. 2563 - 2567 (2008/02/04)
Herein we describe the development of an efficient, safe and practical process for the synthesis of 7-methoxy-2-(2-amino-4-thiazolyl)quinoline. Our new process allowed for a more convergent approach and eliminates the use of potentially dangerous reagents such as diazomethane used in the previous discovery approach. Georg Thieme Verlag Stuttgart.
A novel palladium-catalyzed domino Tsuji - Trost - Heck process for the synthesis of tetrahydroanthracenes
Tietze, Lutz F.,Nordmann, Gero
, p. 3247 - 3253 (2007/10/03)
A novel type of palladium-catalyzed domino reaction is described combining Tsuji - Trost and Heck reactions. This method allows efficient access to tetrahydroanthracene derivatives 1 in up to 89% isolated yield in a one-pot process starting from the diket
Quinolyloxyacetamides
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, (2008/06/13)
Quinoline derivatives of formula: STR1 in which either R 1 denotes trifluoromethyl, R 2 and R 3 form, together with the nitrogen atom to which they are attached, morpholino and R 4 denotes a 4-methylphenyl, 4-chlorophenyl, 2-, 3- or 4-fluorophenyl, 4-meth
Process for the preparation of optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones
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, (2008/06/13)
A new process has been developed for the synthesis of optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones. In particular, the process is particularly adaptable for the preparation of the 5,6-disubstituted compounds, e.g., 5,6-dimethyl-1,2,3,5-tetrahydroimidazo-[2,1-b]quinazolin-2-one. The compounds so prepared are useful as blood platelet anti-aggregative and/or antihypertensive agents in mammals, including humans.
