참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | 4-Methylthiophene-2-boronic acid | HCID 2734373 | — |
| 반응물 | Potassium tert-butoxide | HCID 23665647 | — |
| 반응물 | 4-Bromo-N-[5-(cis-3,5-dimethyl-1-piperazinyl)-2-(methyloxy)phenyl]benzenesulfonamide | HCID 44452776 | — |
| 촉매 | HCID 178418397 | HCID 178418397 | — |
| 용매 | Water | HCID 962 | — |
| 용매 | 1,2-Dimethoxyethane | HCID 8071 | — |
| 생성물 | HCID 59007070 | HCID 59007070 | — |
반응 단계
To a mixture of 4-bromo-N-[5-(cis-3,5-dimethyl-1-piperazinyl)-2-(methyloxy)phenyl]benzenesulfonamide (E106) (100 mg, 0.22 mmol) and (4-methyl-2-thienyl)boronic acid (71 mg, 0.50 mmol) in DME (3 ml) was added potassium tert-butoxide (220 mg, 1.96 mmol) and tetrakis(triphenylphosphine)palladium(0) (15 mg, 0.01 mmol) in water (1 ml) and the resulting mixture stirred in a microwave (set at high absorbance) at 100° C. for 30 minutes. The resulting mixture was then evaporated in vacuo and purified using an SCX cartridge eluting with methanol followed by ammonia (2M in methanol). The appropriate fractions were combined and solvent evaporated in vacuo and the residue purified further by mass directed autoprep HPLC to afford the title compound (E107). MS (ES+) m/e 472 [M+H]+.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US07381728B2 |
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| 출처 데이터셋 | uspto-grants-2008_06 |
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| ORD ID | ord-54c353fc63094d949f46eadf9835d2d8 |
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| 출처 메모 | uspto-grants-2008_06 |
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