4-Chloro-5,7-difluoroquinazoline synthesis
- Product Name:4-Chloro-5,7-difluoroquinazoline
- CAS Number:791602-75-0
- Molecular formula:C8H3ClF2N2
- Molecular Weight:200.57
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Yield:-
Reaction Conditions:
with N-ethyl-N,N-diisopropylamine;trichlorophosphate in acetonitrile at 0 - 80; for 4.75 h;Heating / reflux;
Steps:
5
Phosphoryl chloride (3.32 ml) was added to a stirred mixture of 5,7-difluoro- 3,4-dihydroquinazolin-4-one (5 g), diisopropylethylamine (7.16 ml) and acetonitrile (120 ml)25 that was cooled in an ice bath. The resultant reaction mixture was heated to 800C for 2 hours. A second portion of phosphoryl chloride (1.52 ml) was added and the reaction mixture was heated to reflux for a further 2.75 hours to provide a solution of 4-chloro- 5,7-difiuoroquinazoline which was used without being isolated. A solution of 6-chloro- 2,3-methylenedioxyaniline (International Application WO 01/94341, Example 17, Note [30];30 4.95 g) in acetonitrile (15 ml) was added and the reaction mixture was heated to 80°C for 4 hours. The resultant reaction mixture was stirred at ambient temperature for 16 hours. A solution of a second portion of 6-chloro-2,3-methylenedioxyaniline (1.18 g) in acetonitrile (5 ml) was added and the reaction mixture was reheated to 8O0C for 1 hour. The reaction EPO
References:
WO2006/64217,2006,A2 Location in patent:Page/Page column 54-55