참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Sodium Iodide | HCID 5238 | — |
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | L-Proline | HCID 145742 | — |
| 반응물 | 4'-(3-Bromo-benzyloxy)-4,5-difluoro-2-methoxy-biphenyl | HCID 67153750 | — |
| 촉매 | Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI) | HCID 24350 | — |
| 생성물 | HCID 52920346 | HCID 52920346 | — |
반응 단계
To a vial containing copper(I) iodide (10 mg, 0.050 mmol), sodium iodide (30 mg, 0.2 mmol), cesium carbonate (114 mg, 0.35 mmol) and (S)-pyrrolidine-2-carboxylic acid (14 mg, 0.12 mmol) was added an aliquot of a stock solution of 4′-(3-bromo-benzyloxy)-4,5-difluoro-2-methoxy-biphenyl (1 ml of 0.1M in DMSO). The vial was sealed and heated to 100° C. for 15 hr. The reaction was filtered through Celite and purified by HPLC with increasing concentration of acetonitrile in water with 0.1% trifluoroacetic acid, yielding the product, (S)-1-[3-(4′,5′-difluoro-2′-methoxy-biphenyl-4-yloxymethyl)-phenyl]-pyrrolidine-2-carboxylic acid as an off white solid (11 mg, 25%). LC-MS (ES) calculated for C25H23F2NO4, 439.16; found m/z 440 [M+H]+.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US07939569B1 |
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| 출처 데이터셋 | uspto-grants-2011_05 |
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| ORD ID | ord-705b9bfed6444c87becea8ec85cfd6d6 |
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| 출처 메모 | uspto-grants-2011_05 |
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