Formamide → 6-Methoxy-7-(3-morpholinopropoxy)-3,4-dihydroquinazolin-4-one

Participants

Reaction Steps

WO 01/21594 describes a process for a 6-alkoxy-7-aminoalkoxyquinazolin-4-one compound or a 7-alkoxy-6-aminoalkoxyquinazolin-4-one compound. For instance, ethyl 3-methoxy-4-(3-morpholinopropoxy)-6-aminobenzoate is reacted with formamide to give 6-methoxy-7-(3-morpholinopropoxy)quinazolin-4-one in 68% yield. This process, however, has a problem as an industrially applicable process in that the yield is low, and the teratogenetic formamide is reacted at an elevated temperature in an excessive amount.

Provenance & Evidence