참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | 4-Methylmorpholine | HCID 7972 | — |
| 반응물 | Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphate | HCID 151348 | — |
| 반응물 | Benzyloxycarbonyl-L-methionine | HCID 1550857 | — |
| 반응물 | HCID 68767611 | HCID 68767611 | — |
| 용매 | Dimethylformamide | HCID 6228 | — |
| 생성물 | HCID 21074905 | HCID 21074905 | 97% |
반응 단계
A solution of (1R,2S,5R)-tert-butyl 2-amino-7-oxo-6-aza-bicyclo[3.2.1]octane-6-carboxylate (2.5 g) was dissolved in DMF (34 mL) and cooled to 0° C. prior to the addition of N-Cbz methionine (5.3 g), 4-methyl morpholine (3.7 g), and BOP (8.3 g). The reaction was stirred for 12 h at RT and then partitioned between EtOAc and 1N HCl solution. The organic phases were combined, washed with saturated NaHCO3 and brine, dried (MgSO4), filtered, and concentrated in vacuo. The residue was purified by flash chromatography to afford (1R,2S,5R)-tert-butyl 2-((S)-2-(benzyloxycarbonylamino)-4-(methylthio)butanamido)-7-oxo-6-aza-bicyclo[3.2.1]octane-6-carboxylate (5.1 g). MS found: (M+H)+=506.2.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US07829571B2 |
|---|
| 출처 데이터셋 | uspto-grants-2010_11 |
|---|
| ORD ID | ord-9850ec62580e4e14a3a5e11c23f4789c |
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| 출처 메모 | uspto-grants-2010_11 |
|---|
