反応 #156933

反応方程式

(S)-3-((4-(4-bromophenyl)piperazin-1-yl)methyl)-7,8,9,10-tetrahydro-5H-dipyrido[1,2-a:3′,2′-e]pyrazin-6(6aH)-one

2-methoxypyridin-4-ylboronic acid

sodium bicarbonate

→

(S)-3-((4-(4-(2-methoxypyridin-4-yl)phenyl)piperazin-1-yl)methyl)-7,8,9,10-tetrahydro-5H-dipyrido[1,2-a:3′,2′-e]pyrazin-6(6aH)-one

溶媒

dioxane

反応条件

後処理

1. 1
   その他The aqueous layer was removed from the vial and reaction mixture the
2. 2
   ろ過filtered into a 1.8 mL HPLC submission vial
3. 3
   その他The reaction mixture was purified by LCMS
4. 4
   その他to give a yellow solid

実験手順

(S)-3-((4-(4-bromophenyl)piperazin-1-yl)methyl)-7,8,9,10-tetrahydro-5H-dipyrido[1,2-a:3′,2′-e]pyrazin-6(6aH)-one (0.04 mmol), 2-methoxypyridin-4-ylboronic acid (0.060 mmol), PdCl2(dppf)-CH2Cl2 Adduct (3.27 mg, 4.00 μmol), sodium bicarbonate (0.500 ml, 0.500 mmol), dioxane (Volume: 1 ml) and a stir bar were sealed in a 5 mL microwave vial. The vial was heated to 135° C. for 30 minutes. The aqueous layer was removed from the vial and reaction mixture the filtered into a 1.8 mL HPLC submission vial. The reaction mixture was purified by LCMS to give a yellow solid: [M+H] calc'd for C28H32N6O2, 485; found, 485.

出典