تفاعل #2264479

معادلة التفاعل

Bu3P

[5-(2-fluoro-4-methylphenyl)-3-methyl-1,2-thiazol-4-yl]methanol

ethyl 3-(3,5-difluoro-4-hydroxyphenyl)propanoate

ADDP

→

Ethyl 3-(3,5-difluoro-4-[[5-(2-fluoro-4-methylphenyl)-3-methyl-1,2-thiazol-4-yl]methoxyl]phenyl)propanoate

المذيبات

toluene

ظروف التفاعل

المعالجة

1. 1
   أخرىInto a 25-mL round-bottom flask purged
2. 2
   درجة الحرارةmaintained with an inert atmosphere of nitrogen
3. 3
   تركيزThe resulting mixture was concentrated under vacuum
4. 4
   أخرىThis resulted in 150 mg (79%) of ethyl 3-(3,5-difluoro-4-[[5-(2-fluoro-4-methylphenyl)-3-methyl-1,2-thiazol-4-yl]methoxy]phenyl) propanoate as colorless oil

الإجراء التجريبي

Into a 25-mL round-bottom flask purged and maintained with an inert atmosphere of nitrogen, was placed [5-(2-fluoro-4-methylphenyl)-3-methyl-1,2-thiazol-4-yl]methanol (100 mg, 0.42 mmol, 1.00 equiv), ethyl 3-(3,5-difluoro-4-hydroxyphenyl)propanoate (146 mg, 0.63 mmol, 1.50 equiv), ADDP (221.6 mg, 0.89 mmol, 2.10 equiv), Bu3P (128 mg, 0.63 mmol, 1.5 equiv), toluene (10 mL). The resulting solution was stirred overnight at 60° C. The resulting mixture was concentrated under vacuum. The residue was applied onto a silica gel column with ethyl acetate/petroleum ether (1:5). This resulted in 150 mg (79%) of ethyl 3-(3,5-difluoro-4-[[5-(2-fluoro-4-methylphenyl)-3-methyl-1,2-thiazol-4-yl]methoxy]phenyl) propanoate as colorless oil.

المصدر