تفاعل #332739

معادلة التفاعل

6-((2R,6S)-2,6-dimethylmorpholino)-7-fluoro-3-(furan-2-yl)benzo[d]isoxazole-5-carbaldehyde

Intermediate 427

6-((2R,6S)-2,6-dimethylmorpholino)-7-fluoro-3-(furan-2-yl)benzo[d]isoxazole-5-carbaldehyde

pyrimidine-2,4,6(1H,3H,5H)-trione

→

title compound

المردود 85.0%

(2R,4S,4aS)-rel-11-fluoro-8-(furan-2-yl)-2,4-dimethyl-2,4,4a,6-tetrahydro-1H,1′H-spiro[isoxazolo[4,5-g][1,4]oxazino[4,3-a]quinoline-5,5′-pyrimidine]-2′,4′,6′(3′H)-trione

المردود 85.0%

المذيبات

isopropanol

ظروف التفاعل

المعالجة

1. 1
   أخرىSolvent removed
2. 2
   أخرىResidue was triturated with methanol
3. 3
   ترشيحthe solid was filtered
4. 4
   غسيلwashed with small amount of methanol
5. 5
   أخرىdried

الإجراء التجريبي

A mixture of 6-((2R,6S)-2,6-dimethylmorpholino)-7-fluoro-3-(furan-2-yl)benzo[d]isoxazole-5-carbaldehyde (Intermediate 427, 95 mg, 0.28 mmol) and pyrimidine-2,4,6(1H,3H,5H)-trione (38.9 mg, 0.30 mmol) in isopropanol (10 ml) was heated at 90° C. for 2 days. Solvent removed. Residue was triturated with methanol and the solid was filtered, washed with small amount of methanol, and dried to give title compound (107 mg, 85%).

المصدر