تفاعل #88783

معادلة التفاعل

6-bromo-5-(hydroxy(6-(trifluoromethyl)pyridin-3-yl)methyl)-1-methyl-3-(3-((tetrahydro-2H-pyran-2-yl)oxy)propyl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione

→

3-(6-bromo-1-methyl-2,4-dioxo-5((6-(trifluoromethyl)pyridin-3-yl)methyl)-1,2-dihydropyrido[2,3-d]pyrimidin-3(4H)-yl)propylformate

المردود 57.1%

المذيبات

formic acid

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةcooled to RT
2. 2
   ترشيحfiltered
3. 3
   تركيزThe filtrate was concentrated to a residue which
4. 4
   أخرىwas purified by chromatography
5. 5
   غسيلeluted with PE/EA (10:1)

الإجراء التجريبي

To a stirred solution of 6-bromo-5-(hydroxy(6-(trifluoromethyl)pyridin-3-yl)methyl)-1-methyl-3-(3-((tetrahydro-2H-pyran-2-yl)oxy)propyl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione (160 mg, 0.280 mmol) in formic acid (2 mL) was added Zinc dust (40.9 mg, 0.64 mmol). The reaction was heated at 50° C. for 2 h, cooled to RT and filtered. The filtrate was concentrated to a residue which was purified by chromatography eluted with PE/EA (10:1) to give 3-(6-bromo-1-methyl-2,4-dioxo-5((6-(trifluoromethyl)pyridin-3-yl)methyl)-1,2-dihydropyrido[2,3-d]pyrimidin-3(4H)-yl)propylformate (80 mg, 57.1% yield). LCMS: MH+ 501 and TR=1.727 min.

المصدر