تفاعل #956992

معادلة التفاعل

N-Cyclopropyl-3-fluoro-5-[3-[[1-(2-hydroxyphenyl)cyclopropyl]amino]-2-oxo-1(2H)-pyrazinyl]-4-methyl-benzamide

1-bromo-2-chloroethane

cesium carbonate

→

subtitle compound

3-[3-[[1-[2-(2-chloroethoxy)phenyl]cyclopropyl]amino]-2-oxo-1(2H)-pyrazinyl]-N-cyclopropyl-5-fluoro-4-methyl-benzamide

المذيبات

acetonitrile

ظروف التفاعل

المعالجة

1. 1
   أخرىThe cooled reaction mixture
2. 2
   أخرىwas evaporated to dryness
3. 3
   workup.ADDITIONdiluted with water (500 mL)
4. 4
   استخلاصextracted with dichloromethane (3×300 mL)
5. 5
   تجفيفThe combined organics were dried (MgSO4)
6. 6
   ترشيحfiltered
7. 7
   أخرىevaporated
8. 8
   أخرىThe residue was triturated with 1:1 iso-hexane

الإجراء التجريبي

N-Cyclopropyl-3-fluoro-5-[3-[[1-(2-hydroxyphenyl)cyclopropyl]amino]-2-oxo-1(2H)-pyrazinyl]-4-methyl-benzamide (Preparation 1k, 5 g), 1-bromo-2-chloroethane (9.58 mL) and cesium carbonate (37.5 g) were stirred together in acetonitrile (200 mL) at 80° C. under nitrogen for 16 h. The cooled reaction mixture was evaporated to dryness, diluted with water (500 mL) and extracted with dichloromethane (3×300 mL). The combined organics were dried (MgSO4), filtered and evaporated. The residue was triturated with 1:1 iso-hexane:diethyl ether to give the subtitle compound (4.60 g).

المصدر