Synthesis and biological activity of 4‐methylene‐pyrido[4,3‐d]pyrimidines

Abstract

in Wiley InterScience (www.interscience.wiley.com).Fifteen novel 3-substituted-5-methyl-4-methylene-7-alkylsulfanyl-3,4-dihydro-pyrido [4,3-d]pyrimidine-8-carbonitriles 5a-o, were synthesized via a facile annulation process in which formation of the pyrimidine ring proceeded smoothly by the regioselective attack of a formamidate group on a neighboring carbonyl group instead of a cyano group. Bioassay results indicated that these compounds showed significant herbicidal activity at a dose of 100 lg/mL on the roots of oil rape and barnyard grass. In addition, some of these compounds displayed fungicidal activity.

Access to Fully Substituted Dihydropyrimidines via Dual Copper/Photoredox‐Catalyzed Domino Annulation of Oxime Esters and Imines

“…Dihydropyrimidines and their derivatives are an important class of six‐membered N ‐heterocycles that present in many biologically and medicinally significant molecules, which have diverse biological activities such as anti‐HIV, [1a,b] antihypertensive, [1c] antiviral, [1d,e] anti‐inflammatory, [1f] anticancer, [1g] and antitubercular [1h] activities. Additionally, such compounds are broadly utilized as herbicides [2a] and pesticides [2b] . Therefore, the development of effective synthetic protocols to construct dihydropyrimidine skeletons has attracted great attention in the areas of organic synthesis and drug discovery [3]…”

Developments of pyridodipyrimidine heterocycles and their biological activities

“…Pyridodipyrimidines are a class of nitrogen-bearing heterocycles that established considerable interest owing to their uses in numerous fields [ 8 – 13 ]. The compounds with pyridopyrimidine skeleton demonstrated privileged biological aspects on a large scale such as DHFR inhibitors [ 14 ], EGFr inhibitors [ 14 – 16 ], antitumor [ 17 ], antiviral, anti-inflammatory, and antimicrobial effects [ 18 – 23 ]. This review aims to highlight an example of polycyclic compounds containing the pyrimidine and pyridine cores of distinct biological significance.…”