284486-58-4

Upstream product

• 26059-80-3 2-cyclohexyl-4-hydroxyquinazoline 
• 2719-27-9 cyclohexanylcarbonyl chloride 
• 42468-47-3 2-(cyclohexylcarbonylamino)benzamide 
• 118-92-3 anthranilic acid 
• 766-05-2 cyclohexane carbonitrile 
• 94052-40-1 methyl cyclohexanecarboximidate hydrochloride 
• 26059-80-3 2-cyclohexylquinazolin-4(3Η)-one 
• 28144-70-9 anthranilic acid amide 

Downstream Products

• 284486-53-9 N-(2-cyclohexylquinazol-4-yl)-L-4-(N,N-dimethylcarbamyloxy)phenylalanine tert-butyl ester 
• 1303609-72-4 C₂₄H₂₂N₂O 

Relevant academic research and scientific papers

Fused ring heteroaryl and heterocyclic compounds which inhibit leukocyte adhesion mediated by VLA-4

Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

A facile and versatile route to 2-substituted-4(3H)-quinazolinones and quinazolines

A range of 2-aryl and 2-alkyl quinazolinones have been prepared in moderate to good yields from the reaction of anthranilic acid and the appropriately substituted imidate in a facile, mild, onepot procedure. Subsequent reaction with phosphorus oxychloride afforded the corresponding 4-chloro-2-substituted quinazolines, which are useful synthetic intermediates, in good to high yields. Product isolation was facilitated by the development of work up procedures for both reactions that did not include purification by column chromatography.

Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities

Moderate cyclic GMP phosphodiesterase (cGMP-PDE, PDE V) inhibitor 2- phenyl-4-anilino-quinazoline (1) was identified utilizing MultiCASE assisted drug design (MCADD) technology. Modification of compound 1 was conducted at the 2-, 4-, and 6-positions of the quinazoline ring for enhancement of cGMP- PDE inhibitory activity. The 6-substituted 2-(imidazol-1-yl)-quinazolines are 1000 times more potent in in vitro PDE V enzyme assay than the well-known inhibitor zaprinast. The 6-substituted derivatives of 2-(3- pyridyl)quinazoline 84 and 2-(imidazol-1-yl)quinazoline 86 exhibited more than 1000-fold selectivity for PDE V over the other four PDE isozymes. In addition, cGMP-PDE inhibitors 64, 65, and 73 were found to have an additional property of thromboxane synthesis inhibitory activity.