تفاعل #47906

معادلة التفاعل

6-Benzyl-4-chloro-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine

6-trifluoromethylpyridin-3-ylamine

HI H2O

→

product

المردود 95.0%

6-Benzyl-N-(6-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-amine

المردود 95.0%

المذيبات

dioxane

ظروف التفاعل

المعالجة

1. 1
   أخرىThe solvents were removed under vacuum
2. 2
   workup.DISSOLUTIONthe residue was dissolved in ethyl acetate
3. 3
   غسيلwashed with sat. NaHCO3 and brine
4. 4
   تجفيفThe organic layer was dried over Na2SO4
5. 5
   ترشيحfiltered
6. 6
   أخرىevaporated

الإجراء التجريبي

6-Benzyl-4-chloro-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine (0.5 g, 1.93 mmol) was dissolved in anhydrous dioxane (3 mL) and 6-trifluoromethylpyridin-3-ylamine was added (469 mg, 2.9 mmol), followed by HI/H2O (0.3 mL, 47%). The mixture was heated at 130° C. for 600 s in a Personal Chemistry microwave. The solvents were removed under vacuum and the residue was dissolved in ethyl acetate and washed with sat. NaHCO3 and brine. The organic layer was dried over Na2SO4, filtered and evaporated to give the product as an orange solid (700 mg, 95% crude). The crude product was used for the subsequent step.

المصدر