Bromotrimethylsilane → (1S,5S)-(1-{5-[(4-amino-benzenesulfonyl)-isobutyl-amino]-6-phosphonooxy hexylcarbamoyl}-2,2-diphenyl-ethyl)-carbamic acid methyl ester

HRID 2041619

반응식

HRID 2041619 반응식
[CH3:1][O:2][C:3](=[O:52])[NH:4][C@H:5]([C:19](=[O:51])[NH:20][CH2:21][CH2:22][CH2:23][CH2:24][C@H:25]([N:36]([S:41]([C:44]1[CH:49]=[CH:48][C:47]([NH2:50])=[CH:46][CH:45]=1)(=[O:43])=[O:42])[CH2:37][CH:38]([CH3:40])[CH3:39])[CH2:26][O:27][P:28]([O:33]CC)([O:30]CC)=[O:29])[CH:6]([C:13]1[CH:18]=[CH:17][CH:16]=[CH:15][CH:14]=1)[C:7]1[CH:12]=[CH:11][CH:10]=[CH:9][CH:8]=1.C[Si](Br)(C)C>ClCCl>[CH3:1][O:2][C:3](=[O:52])[NH:4][C@H:5]([C:19](=[O:51])[NH:20][CH2:21][CH2:22][CH2:23][CH2:24][C@H:25]([N:36]([S:41]([C:44]1[CH:45]=[CH:46][C:47]([NH2:50])=[CH:48][CH:49]=1)(=[O:42])=[O:43])[CH2:37][CH:38]([CH3:40])[CH3:39])[CH2:26][O:27][P:28]([OH:33])([OH:30])=[O:29])[CH:6]([C:13]1[CH:18]=[CH:17][CH:16]=[CH:15][CH:14]=1)[C:7]1[CH:8]=[CH:9][CH:10]=[CH:11][CH:12]=1

참가 물질

4

반응물 2

HCID 76113BromotrimethylsilaneHCID 24778259(1S,5S)-{1-[5-[(4-amino-benzenesulfonyl)-isobutyl-amino]-6-(diethoxy-phosphoryloxy)-hexylcarbamoyl]-2,2-diphenyl-ethyl}-carbamic acid methyl ester

생성물 1

HCID 11563875(1S,5S)-(1-{5-[(4-amino-benzenesulfonyl)-isobutyl-amino]-6-phosphonooxy hexylcarbamoyl}-2,2-diphenyl-ethyl)-carbamic acid methyl ester

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

The product of step G prepared above (152 mg) was dissolved in anhydrous dichloromethane (3.0 mL). Trimethylsilyl bromide (0.5 mL) was added at 0° C. The mixture was stirred during 1 h at this temperature and overnight at room temperature. The solvent was evaporated and 0.2 mL water was added to the residue. 3 mL EtOH was added mixed and evaporated. This step was repeated three times and the residue dried in vacuo. Yields 98 mg 70% of the title derivatives of this first example.

후처리

  1. customThe solvent was evaporated
  2. addition0.2 mL water was added to the residue
  3. addition3 mL EtOH was added
  4. additionmixed
  5. customevaporated
  6. customthe residue dried in vacuo
  7. customYields 98 mg 70% of the title derivatives of this first example

출처 및 근거

ORD 기록
ord-f0f3827022d74760924a84f265c08e79
출처 데이터셋
uspto-grants-2013_11
특허 번호
US08580995B2

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