159237-77-1

Upstream product

• 26177-44-6 4-bromobenzylamine hydrochloride 
• 159237-73-7 4-chloro-2,6-dimethyl-5-(1-ethoxyvinyl)pyrimidine 
• 71-36-3 butan-1-ol 
• 83410-37-1 5-iodo-2,6-dimethyl-pyrimidin-4-ol 
• 6622-92-0 4-hydroxy 2,6-dimethylpyrimidine 
• 83410-16-6 4-chloro-5-iodo-2,6-dimethylpyrimidine 

Downstream Products

• 159237-74-8 methyl(4-(4-bromobenzylamino)-2,6-dimethylpyrimidin-5-yl)ketone 
• 1027898-62-9 1-(4-{[2'-(2-tert-Butyl-2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-2,6-dimethyl-pyrimidin-5-yl)-ethanone 

Relevant academic research and scientific papers

Metabolites of the angiotensin II antagonist tasosartan: The importance of a second acidic group

Described in this paper is the synthesis and pharmacological activity of five metabolites of the angiotensin II antagonist tasosartan (1). Of particular interest is the effect of the additional acidic group of the enol metabolite (8) on activity. As suggested by the structural-activity relationship of other angiotensin II antagonist series, a second acidic group can improve receptor binding activity but decrease in vivo activity after oral dosing. The metabolic introduction of a second acidic group in tasosartan bypasses this problem and contributes to the excellent profile of the compound. A molecular modeling study provides a rationale for the role of the enol group of 8 in AT1 receptor binding.

Substituted pyridopyrimidines and antihypertensives

This invention relates to substituted pyridopyrimidinones of general formula (I): STR1 wherein R1 and R2 are independently H, lower alkyl containing 1 to 6 carbon atoms, hydroxyalkyl containing 1 to 6 carbon atoms, formyl, carbonylalkyl containing 1 to 6 carbon atoms, carboxy, or carboxyalkyl containing 1 to 6 carbon atoms; R3 and R4 are independently H, lower alkyl containing 1 to 6 carbon atoms, hydroxy; R3a and R4a are H, and when taken together with R3 and R4 respectively comprise a carbonyl; with the proviso that at least one of the groups R1 and R2 must be hydroxyalkyl, formyl, carbonylalkyl containing 1 to 6 carbon atoms, carboxy, or carboxyalkyl containing 1 to 6 carbon atoms; or R3 and R4 must be hydroxy or taken together with R3a and R4a respectively must comprise a carbonyl; n is 0 to 3; Ar1 is STR2 wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; Ar2 is STR3 wherein X is CO2 H, CN, or STR4 wherein R5 is H, CH3, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereofuseful for treating hypertension and congestive heart failure, to pharmaceutical compositions, and to methods for production thereof.