A2B ADENOSINE RECEPTOR ANTAGONISTS
Disclosed are processes for the synthesis of novel compounds that are A 2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
1 . An intermediate of the formula:
wherein:
R 1 and R 2 are independently chosen from methyl, ethyl, n-propyl, 2-methylpropyl, and cyclopropylmethyl.
2 . The intermediate of claim 1 , wherein R 1 is n-propyl and R 2 is ethyl:
namely 6-[2-(dimethylamino)-1-azavinyl]-1-ethyl-3-propyl-1,3-dihydropyrimidine-2,4-dione.
3 . An intermediate of the formula:
wherein R 1 is n-propyl or cyclopropylmethyl.
4 . The intermediate of claim 3 , wherein R 1 is n-propyl:
namely N-(6-amino-2,4-dioxo-3-propyl(1,3-dihydropyrimidin-5-yl))(1-{[3-(trifluoromethyl)-phenyl]methyl}pyrazol-4-yl)carboxamide.
5 . An intermediate of the formula:
wherein R 2 is methyl or ethyl.
6 . The intermediate of claim 5 , wherein R 2 is ethyl:
N-(6-amino-1-ethyl-2,4-dioxo(1,3-dihydropyrimidin-5-yl))(1-{{[3-(trifluoromethyl)phenyl]methyl}pyrazol-4-yl)carboxamide.
7 . An intermediate of the formula:
wherein R 1 and R 2 are independently chosen from methyl, ethyl, n-propyl, 2-methylpropyl, and cyclopropylmethyl.