تفاعل #49043

معادلة التفاعل

3,4-Difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-5-[(2-hydroxy-ethoxyamino)-methyl]-benzamide

3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-5-[(2-hydroxy-ethoxyamino)-methyl]-benzamide

N,N′-disuccinimidyl carbonate

NEt3

→

title compound

المردود 11.9%

3,4-Difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-5-(3-oxo-[1,4,2]dioxazinan-2-ylmethyl)-benzamide

المردود 11.9%

المذيبات

CH2Cl2 THF

ظروف التفاعل

المعالجة

1. 1
   أخرىThe reaction mixture was purified by silica gel column chromatography (CH2Cl2/MeOH as a developing solvent)

الإجراء التجريبي

3,4-Difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-5-[(2-hydroxy-ethoxyamino)-methyl]-benzamide (100 mg, 0.185 mmol) obtained in Example 6, N,N′-disuccinimidyl carbonate (59 mg, 0.231 mmol) and NEt3 (113 mg, 1.12 mmol) were stirred in a mixed solvent of CH2Cl2/THF (1 mL/1 mL) at room temperature for 10 hours. The reaction mixture was purified by silica gel column chromatography (CH2Cl2/MeOH as a developing solvent) to give the title compound (12.5 mg).

المصدر