A convenient synthesis of novel 5-aryl-pyrido[2,3-d]pyrimidines and screening of their preliminary antibacterial properties

作者：Saikia Lakhinath; Das Babulal; Bharali Pranjal; Thakur Ashim Jyoti^*

来源：Tetrahedron Letters, 2014, 55(10): 1796-1801.

DOI：10.1016/j.tetlet.2014.01.128

• Uracil
• Pyrido[2,3-d]pyrimidine
• Amidine
• Antibacterial
• Diels-Alder

Exploiting the diene nature of 6[1-aza-2-(dimethylamino)prop-l-enyl]-1,3-dimethyluracil (2), novel 5-aryl-pyrido[2,3-d]pyrimidines (5a-h) have been synthesized. The reaction proceeds through a triene intermediate whose structure has been conclusively established by single crystal X-ray analysis. Role of water is intriguing as the reaction can be stopped at the intermediate stage. Synthesized compounds have been screened for possible antibacterial properties and results showed modest activity.

• 出版日期2014-3-5