Azetidine → {3-[3-(Azetidin-1-yl)-1,2,4-oxadiazol-5-yl]-5-(4-ethylphenyl)piperidin-1-yl}(4-hydroxypiperidin-1-yl)methanone

HRID 661280노트

반응식

HRID 661280 반응식
Cl[C:2]1[N:6]=[C:5]([CH:7]2[CH2:12][CH:11]([C:13]3[CH:18]=[CH:17][C:16]([CH2:19][CH3:20])=[CH:15][CH:14]=3)[CH2:10][N:9]([C:21]([N:23]3[CH2:28][CH2:27][CH:26]([OH:29])[CH2:25][CH2:24]3)=[O:22])[CH2:8]2)[O:4][N:3]=1.[NH:30]1[CH2:33][CH2:32][CH2:31]1>C(O)C>[N:30]1([C:2]2[N:6]=[C:5]([CH:7]3[CH2:12][CH:11]([C:13]4[CH:18]=[CH:17][C:16]([CH2:19][CH3:20])=[CH:15][CH:14]=4)[CH2:10][N:9]([C:21]([N:23]4[CH2:28][CH2:27][CH:26]([OH:29])[CH2:25][CH2:24]4)=[O:22])[CH2:8]3)[O:4][N:3]=2)[CH2:33][CH2:32][CH2:31]1

참가 물질

4

반응물 2

HCID 10422AzetidineHCID 58116548[3-(3-Chloro-1,2,4-oxadiazol-5-yl)-5-(4-ethylphenyl)piperidin-1-yl](4-hydroxypiperidin-1-yl)-methanone

생성물 1

HCID 49819562{3-[3-(Azetidin-1-yl)-1,2,4-oxadiazol-5-yl]-5-(4-ethylphenyl)piperidin-1-yl}(4-hydroxypiperidin-1-yl)methanone

시약·촉매·용매 1

HCID 702Ethanol용매

실험 절차

To a solution of 80.0 mg (0.174 mmol) of the oxadiazole from Example 25A in 1.10 ml of ethanol were added 198 mg (3.48 mmol) of azetidine, and then the reaction mixture was stirred in the microwave at 80 for 2 h. The solvent was removed under reduced pressure and the crude product was purified by means of preparative HPLC. Yield: 46.9 mg (61% of theory)

후처리

  1. customThe solvent was removed under reduced pressure
  2. customthe crude product was purified by means of preparative HPLC

출처 및 근거

ORD 기록
ord-c37935ac9b424aba94d2c48296c3b609
출처 데이터셋
uspto-grants-2011_12
특허 번호
US08084469B2

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