PROCESS FOR PREPARING [(3-HYDROXYPYRIDINE-2-CARBONYL)AMINO]ALKANOIC ACIDS, ESTERS AND AMIDES

摘要

Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.

主权项

1. A compound having the formula: wherein A is a ring chosen from: i) C6 or C10 aryl; or ii) C1-C9 heteroaryl; R10 units represent at least one optionally present substitutions for a ring hydrogen atom; or two R10 units can be taken together to form a substituted or unsubstituted C4-C8 cycloalkyl ring, a substituted or unsubstituted C6 or C10 aryl ring, a substituted or unsubstituted C2-C8 heterocyclic ring, or a substituted or unsubstituted C3 to C5 heteroaryl ring, wherein the heterocyclic and heteroaryl rings comprise one or more hetero atoms independently chosen from oxygen (O), nitrogen (N), or sulfur (S).