تفاعل #45163

معادلة التفاعل

trimethylaluminium

ethyl 4-(4-cyclopropyl-1,4-diazepan-1-yl)benzoate

5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-amine

DCM Ether

→

title compound

المردود 33.7%

4-(4-cyclopropyl-1,4-diazepan-1-yl)-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]benzamide

المردود 33.7%

المذيبات

toluene

ظروف التفاعل

المعالجة

1. 1
   أخرى4-(4-cyclopropyl-1,4-diazepan-1-yl)-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]benzamide was prepared
2. 2
   أخرىThe crude product was purified by preparative HPLC
3. 3
   workup.ADDITIONFractions containing the desired compound
4. 4
   أخرىwere evaporated to dryness
5. 5
   أخرىto afford a gum which

الإجراء التجريبي

4-(4-cyclopropyl-1,4-diazepan-1-yl)-N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]benzamide was prepared using the same procedure as for Example 159, but starting from ethyl 4-(4-cyclopropyl-1,4-diazepan-1-yl)benzoate (0.288 g, 1 mmol, 5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-amine (0.247 g, 1 mmol) and a 2M solution of trimethylaluminium (1.250 mL, 2.50 mmol) in toluene. The crude product was purified by preparative HPLC, using decreasingly polar mixtures of water (containing 1% NH3) and MeCN as eluents. Fractions containing the desired compound were evaporated to dryness to afford a gum which solidified on trituration with DCM/Ether to afford the title compound (0.165 g, 33.7%).

المصدر