تفاعل #88706

معادلة التفاعل

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

→

3-(5-(4-chlorobenzyl)-6-((5-chloropyridin-3-yl)oxy)-1-methyl-2,4-dioxo-1,2-dihydropyrido[2,3-d]pyrimidin-3(4H)-yl)propyl formate

المردود 38.0%

المذيبات

HCOOH

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةcooled to RT
2. 2
   ترشيحfiltered
3. 3
   تركيزThe filtrate was concentrated

الإجراء التجريبي

To a solution of 5-((4-chlorophenyl)(hydroxy)methyl)-6-((5-chloropyridin-3-yl)oxy)-1-methyl-3-(3-((tetrahydro-2H-pyran-2-yl)oxy)propyl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione (120 mg, 0.204 mmol) in HCOOH (5 mL) was added Zn dust (66.8 mg, 1.02 mmol). The reaction was heated at 70° C. for 1.5 h, cooled to RT and filtered. The filtrate was concentrated to give 3-(5-(4-chlorobenzyl)-6-((5-chloropyridin-3-yl)oxy)-1-methyl-2,4-dioxo-1,2-dihydropyrido[2,3-d]pyrimidin-3(4H)-yl)propyl formate (40 mg, 38.0% yield) as an oil. LCMS MH+ 515 and TR=1.696 min. Used without further purification.

المصدر