참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Dimethylamine | HCID 674 | — |
| 반응물 | 1,4-Diazabicyclo(2.2.2)octane--trimethylalumane (1/2) | HCID 16688366 | — |
| 반응물 | 7-(4-Benzyl-piperazin-1-yl)-benzofuran-2-carboxylic acid ethyl ester | HCID 59636745 | — |
| 용매 | Tetrahydrofuran | HCID 8028 | — |
| 용매 | Sodium chloride; water | HCID 57417360 | — |
| 생성물 | 7-(4-benzylpiperazin-1-yl)-N,N-dimethylbenzofuran-2-carboxamide | HCID 59636770 | 87.7% |
반응 단계
7-(4-Benzyl-piperazin-1-yl)-benzofuran-2-carboxylic acid ethyl ester (1.0 g, 2.74 mmol) and DABAL-Me3 (0.56 g, 2.20 mmol) were mixed in tetrahydrofuran (5 mL). Dimethylamine (2M in THF) (2.2 mL, 4.39 mmol) was added and the mixture was heated by microwave irradiation to 120° C. for 15 min. Brine was added and the mixture was extracted with dichloromethane, dried over Na2SO4, filtered and the solvent removed by rotary evaporation. The product was purified by flash chromatography (SiO2; DCM/MeOH; gradient 0-2%) giving 7-(4-benzylpiperazin-1-yl)-N,N-dimethylbenzofuran-2-carboxamide (0.70 g, 1.93 mmol) in 70% yield.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US08859534B2 |
|---|
| 출처 데이터셋 | uspto-grants-2014_10 |
|---|
| ORD ID | ord-fad5ab25af9f4a149521755b80ec1b68 |
|---|
| 출처 메모 | uspto-grants-2014_10 |
|---|
