تفاعل #649490

معادلة التفاعل

3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(5-formyl-3-thienyl)-1H-indole-7-carboxamide

(2S)-2-(trifluoromethyl)pyrrolidine

MeOH

sodium borohydride

→

title compound

المردود 8.0%

3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(5-{[(2S)-2-(trifluoromethyl)-1-pyrrolidinyl]methyl}-3-thienyl)-1H-indole-7-carboxamide trifluoroacetate

المردود 8.0%

المذيبات

DCM

ظروف التفاعل

المعالجة

1. 1
   workup.STIRRINGthe reaction was stirred overnight at room temperature
2. 2
   أخرىThe reaction mixture was purified by Gilson Preparatory HPLC

الإجراء التجريبي

To a solution of 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(5-formyl-3-thienyl)-1H-indole-7-carboxamide (50 mg, 0.112 mmol) in DCM (3.0 mL) and MeOH (1.5 mL) was added (2S)-2-(trifluoromethyl)pyrrolidine (156 mg, 1.12 mmol) and acetic acid (5 drops). After 6 h of stirring at room temperature, sodium borohydride (43 mg, 1.12 mmol) was added and the reaction was stirred overnight at room temperature. The reaction mixture was purified by Gilson Preparatory HPLC to give 5.0 mg of the title compound (8%).

المصدر