- Substituent Electronegativity and Isostructurality in the Polymorphism of Clonixin Analogues
-
To gain understanding of how the variation in local weak interactions influences intermolecular interactions and subsequent crystal packing, four analogues of 2-(3-chloro-2-methyl-phenylamino)-nicotinic acid [clonixin] were synthesized by replacing the ch
- Liu, Meng,Shen, Guowen,Yuan, Zhong,Parkin, Sean,Yu, Faquan,Zhang, Mingtao,Long, Sihui,Li, Tonglei
-
-
Read Online
- Synthesis of 2-(arylamino)nicotinic acids in high-temperature water
-
In hydrothermal reactions at 150-180 °C, 2-(arylamino)nicotinic acids were synthesized by amination of 2-chloronicotinic acid with aromatic amine derivatives, with potassium carbonate as base. The procedure is efficient, environmentally friendly, and practical, with moderate to excellent yields (up to 98%). Springer Science+Business Media B.V. 2012.
- Li, Zhenghua,Xiao, Shangyou,Liang, Ronghui,Xia, Zhining
-
p. 1691 - 1697
(2012/10/29)
-
- Catalyst-free amination of 2-chloronicotinic acid in water under microwave irradiation
-
A simple, efficient and environmental friendly method for the synthesis of 2-arylaminonicotinic acids derivatives by reacting 2-chloronicotinic acid with anilines with potassium carbonate as the base and water as the media under microwave irradiation is described. The synthesis of 2-arylaminonicotinic acids is important because they are nonsteroidal anti-inflammatory drugs.
- Li, Zheng-Hua,Xia, Zhi-Ning,Chen, Gang
-
experimental part
p. 709 - 711
(2012/03/09)
-
- Antiallergy Agents. 1. Substituted 1,8-Naphthyridin-2(1H)-ones as Inhibitors of SRS-A Release
-
A novel class of antiallergy agents, the substituted 1,8-naphthyridin-2(1H)-ones, is described.The present compounds are orally active, potent inhibitors of allergic and nonallergic bronchospasm in animal models.Structure-activity studies of the lead compound in this sereis, 1-phenyl-3-n-butyl-4-hydroxynaphthyridin-2(1H)-one (11), identified three compounds of interest, 1-phenyl-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one (12), 1-(3'-chlorophenyl)-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one (87), and 1-(3'-methoxyphenyl)-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one (89).The mechanism of antiallergy activity may involve inhibition of the release of the sulfidopeptide leukotrienes. 1-Phenyl-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one, Sch 33303 (12), was selected for preclinical development as an antiallergy agent.
- Sherlock, Margaret H.,Kaminski, James J.,Tom, Wing C.,Lee, Joe F.,Wong, Shing-Chun,et al.
-
p. 2108 - 2121
(2007/10/02)
-