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HCID 68713472, 화합물 → HCID 59201461, 화합물

HRID 451897
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HRID 451897 반응식
[CH:1]1([CH2:7][C@H:8]([NH:19][C:20]([N:22]2[CH2:27][CH2:26][CH2:25][C@@H:24]([C@H:28]([C:37]3[CH:42]=[C:41]([F:43])[CH:40]=[C:39]([F:44])[C:38]=3[OH:45])[O:29][CH2:30][CH2:31][NH:32][C:33](=[O:36])[O:34][CH3:35])[CH2:23]2)=[O:21])[CH2:9][N:10](C)[C:11](OC(C)(C)C)=O)[CH2:6][CH2:5][CH2:4][CH2:3][CH2:2]1>CO.[Pd]>[CH:1]1([CH2:7][C@H:8]([NH:19][C:20]([N:22]2[CH2:27][CH2:26][CH2:25][C@@H:24]([C@H:28]([C:37]3[CH:42]=[C:41]([F:43])[CH:40]=[C:39]([F:44])[C:38]=3[OH:45])[O:29][CH2:30][CH2:31][NH:32][C:33](=[O:36])[O:34][CH3:35])[CH2:23]2)=[O:21])[CH2:9][NH:10][CH3:11])[CH2:2][CH2:3][CH2:4][CH2:5][CH2:6]1
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참가 물질

4

반응물 1

HCID 68713472HCID 68713472, 화합물

생성물 1

HCID 59201461HCID 59201461, 화합물수율 28.2%

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 887Methanol용매

실험 절차

methyl 2-((R)—((R)-1-((S)-1-cyclohexyl-3-(N-methyl-N-(tert-butoxycarbonyl)amino)propan-2-ylcarbamoyl)piperidin-3-yl)(3,5-difluoro-2-hydroxyphenyl)methoxy)ethylcarbamate (100 mg, 0.131 mmol) was dissolved in MeOH (1 mL) and Pd/C (20 mg) was added to it. The reaction mixture was stirred in 30 psi at room temperature for 2 h. The suspension was filtered and the filtrate was concentrated in vacuo. The residue was purified by preparative HPLC to afford methyl 2-((R)—((R)-1-((S)-1-cyclohexyl-3-(methylamino)propan-2-ylcarbamoyl)piperidin-3-yl)(3,5-difluoro-2-hydroxyphenyl)methoxy)ethylcarbamate (20 mg, 28%).

후처리

  1. filtrationThe suspension was filtered
  2. concentrationthe filtrate was concentrated in vacuo
  3. customThe residue was purified by preparative HPLC

출처 및 근거

ORD 기록
ord-8de695f088bd4b878103f67b5fcbd3a6
출처 데이터셋
uspto-grants-2013_07
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08487108B2

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