تفاعل #66852

معادلة التفاعل

suspension

7-[(2E)-4-Chlorobut-2-enoyl]-N-(3,4-dichlorophenyl)-5,6,7,8-tetrahydropyrido[4′,3′:4,5]thieno[2,3-d]pyrimidin-4-amine

azetidine

→

title compound

المردود 13.1%

7-[(2E)-4-Azetidin-1-ylbut-2-enoyl]-N-(3,4-dichlorophenyl)-5,6,7,8-tetrahydropyrido[4′,3′:4,5]thieno[2,3-d]pyrimidin-4-amine

المردود 13.1%

المذيبات

methyl tert-butyl ether

DMF

ظروف التفاعل

المعالجة

1. 1
   غسيلwashed with water
2. 2
   تجفيفdried over sodium sulfate
3. 3
   أخرىThe solvent was removed in vacuo
4. 4
   أخرىthe residue was purified by preparative HPLC

الإجراء التجريبي

To a suspension of Example 59A (100 mg, 0.20 mmol) in DMF (2 mL) was added azetidine (23 mg, 0.40 mmol), and the mixture was heated to 50° C. for 1 h. It was then diluted with methyl tert-butyl ether, washed with water and dried over sodium sulfate. The solvent was removed in vacuo, and the residue was purified by preparative HPLC to yield 12.4 mg (13%) of the title compound.

المصدر