تفاعل #84052

معادلة التفاعل

6-bromo-1-benzothiophene-2-amine

pentafluorophenyl (1-azabicyclo[2.2.2]oct-3-yl)acetate hydrochloride

hydrochloric acid

carbonate

→

title compound

2-(1-Azabicyclo[2.2.2]oct-3-yl)-N-(6-bromo-1-benzothien-2-yl)acetamide hydrochloride

المذيبات

DMF

acetonitrile

ظروف التفاعل

المعالجة

1. 1
   workup.WAITAfter 3 h
2. 2
   ترشيحthe polystyrene resin is filtered off
3. 3
   غسيلwashed with THF
4. 4
   تركيزThe combined filtrates are concentrated in vacuo
5. 5
   أخرىthe crude product is purified by preparative HPLC
6. 6
   أخرىThe hydrochloride is prepared
7. 7
   workup.ADDITIONby mixing the product
8. 8
   تركيزagain concentrating
9. 9
   أخرىDrying under high vacuum

الإجراء التجريبي

89.2 mg (0.24 mmol) of pentafluorophenyl (1-azabicyclo[2.2.2]oct-3-yl)acetate hydrochloride are dissolved in 1 ml of DMF, mixed with 71.2 mg (0.31 mmol) of 6-bromo-1-benzothiophene-2-amine and stirred at room temperature overnight. 1 g of MP-carbonate (polymer-bound carbonate, capacity: 2.5-3.5 mmol/g; from Argonaut Technologies, USA) is added. After 3 h, the polystyrene resin is filtered off and washed with THF. The combined filtrates are concentrated in vacuo, and the crude product is purified by preparative HPLC. The hydrochloride is prepared by mixing the product with a mixture of 1 M hydrochloric acid and acetonitrile and again concentrating. Drying under high vacuum results in 14 mg (14% of theory) of the title compound.

المصدر