تفاعل #69309

معادلة التفاعل

Water

(3aSR,10RS)-2-(2-Bromo-ethyl)-6-chloro-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione

sodium carbonate

azetidine

→

ammonia

diisopropylether

title compound

(3aSR,10RS)-2-(2-Azetidin-1-yl-ethyl)-6-chloro-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione

المذيبات

acetonitrile

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةThe mixture is heated
2. 2
   درجة الحرارةto reflux for 4 h
3. 3
   استخلاصthe mixture is extracted with ethyl acetate
4. 4
   تجفيفThe organic layer is dried with magnesium sulfate
5. 5
   أخرىThe solvent is removed under reduced pressure

الإجراء التجريبي

To a solution of 200 mg (3aSR,10RS)-2-(2-Bromo-ethyl)-6-chloro-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione (example 26) in 5 ml acetonitrile are added 87 mg sodium carbonate and 83 μl azetidine. The mixture is heated to reflux for 4 h. Water is added and the mixture is extracted with ethyl acetate. The organic layer is dried with magnesium sulfate. The solvent is removed under reduced pressure. After column chromatography (silica gel; ethyl acetate, methanol, ammonia 10:0.2:0.1) and trituration with diisopropylether, 61 mg of the title compound are obtained as a colorless solid. MS: m/z (MH+)=465.1

المصدر