تفاعل #303375

معادلة التفاعل

3-{6-[2-(3,4-Dimethoxy-phenyl)-ethylamino]-2-methanesulfonyl-pyrimidin-4-yloxy}-benzoic acid ethyl ester

3-{6-[2-(3,4-dimethoxy-phenyl)-ethylamino]-2-methanesulfonyl-pyrimidin-4-yloxy}-benzoic acid ethyl ester

Intermediate ( 72 )

3-{6-[2-(3,4-dimethoxy-phenyl)-ethylamino]-2-methanesulfonyl-pyrimidin-4-yloxy}-benzoic acid ethyl ester

sodium methoxide

→

3-{6-[2-(3,4-dimethoxy-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yloxy}-benzoic acid methyl ester

المردود 44.0%

المذيبات

1,2-dimethoxyethane

ظروف التفاعل

المعالجة

1. 1
   ترشيحthe mixture is filtered through a plug of SiO2 (EtOAc)
2. 2
   تركيزThe filtrate is concentrated

الإجراء التجريبي

To a solution of above 3-{6-[2-(3,4-Dimethoxy-phenyl)-ethylamino]-2-methanesulfonyl-pyrimidin-4-yloxy}-benzoic acid ethyl ester [180 mg, 0.36 mmol, Intermediate (72)] in 1,2-dimethoxyethane (5 mL) is added a 25% solution of sodium methoxide (3 mL). After 1 h at 20° C., the mixture is filtered through a plug of SiO2 (EtOAc). The filtrate is concentrated to give 3-{6-[2-(3,4-dimethoxy-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yloxy}-benzoic acid methyl ester [70 mg, 44%, Example (63)]. LCMS: RT=3.34 minutes, MS: 440 (M+H). IC50=6254 nM

المصدر