تفاعل #49605

معادلة التفاعل

tri(o-tolyl)phosphine

triethylamine

4-chloro-5-(2,3-epoxypropoxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)methylindol-2-yl]isoindolinone

→

4-chloro-5-(2,3-epoxypropoxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone

المردود 79.2%

المذيبات

acetonitrile

ظروف التفاعل

المعالجة

1. 1
   أخرىfollowed by purification by slurry

الإجراء التجريبي

In a similar manner to Step 2 of Example 1, 4-chloro-5-(2,3-epoxypropoxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)methylindol-2-yl]isoindolinone (77.1 mg, 0.211 mmol) was dissolved in acetonitrile (2.3 mL), and the solution was treated with Compound BD (151 mg, 0.383 mmol), palladium acetate (3.8 mg, 0.017 mmol), tri(o-tolyl)phosphine (10.3 mg, 0.034 mmol) and triethylamine (0.294 mL, 2.11 mmol), followed by purification by slurry using diisopropylether to obtain 4-chloro-5-(2,3-epoxypropoxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone (92.3 mg, yield 79%).

المصدر