4.4 Article

Synthesis of 2,4-Diaminoquinazoline and 2,4-Diaminopyrido-[2,3-d]pyrimidine Derivatives

Journal

CHINESE JOURNAL OF ORGANIC CHEMISTRY
Volume 34, Issue 2, Pages 414-418

Publisher

SCIENCE PRESS
DOI: 10.6023/cjoc201307028

Keywords

2,4-diaminoquinazoline; 2,4-diaminopyrido[2,3-d]pyrimidine; acylation reaction; synthesis

Funding

  1. National High Technology Research and Development Program of China (863 Program) [2013AA064102]
  2. Project of Science and Technology of Hunan Province [2010FJ4112]

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In this work, several 2,4-diaminoquinazoline and 2,4-diaminopyrido[2,3-d]pyrimidine derivatives were designed and synthesized by acylation reaction and ring-closure reaction, using 6-chloro-5-cyanonicotinic acid, 3-cyano-4-fluorobenzoic acid, 4-cyano-3-fluorobenzoic acid and 6-chloro-5-cyanopicolinic acid as starting materials. This method is simple and efficient. For the used acids but 6-chloro-5-cyanopicolinic acid, the reaction yields are above 65%. The structures of terminational compounds were determined by H-1 NMR, C-13 NMR and LC-MS. The antitumor activities of the nitrogen mustard-linked chalcones were evaluated by an MTT assay. The results reveal that some of the title compounds exhibit potent anti-proliferative activities against selected tumor cells. Among which, compounds 4c, 4d, 4e and 4f against K562 and HepG2 were better than 5-fluorouracil.

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