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3-Iodobenzoic acid → 2-hydroxy-N-[4-(5-oxo-4H-1,2,4-oxadiazol-3-yl)phenyl]-2-[4-(p-tolylsulfonyl)morpholin-2-yl]acetamide

HRID 876621
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HRID 876621 반응식
[OH:1][CH:2]([CH:6]1[O:11][CH2:10][CH2:9][N:8]([S:12]([C:15]2[CH:20]=[CH:19][C:18]([CH3:21])=[CH:17][CH:16]=2)(=[O:14])=[O:13])[CH2:7]1)[C:3]([OH:5])=O.[NH2:22][C:23]1[CH:28]=[CH:27][C:26]([C:29]2[NH:30][O:31][C:32](=[O:34])[N:33]=2)=[CH:25][CH:24]=1.IC1C=C(C=CC=1)C(O)=O.FC1(F)CCNCC1>>[OH:1][CH:2]([CH:6]1[O:11][CH2:10][CH2:9][N:8]([S:12]([C:15]2[CH:20]=[CH:19][C:18]([CH3:21])=[CH:17][CH:16]=2)(=[O:14])=[O:13])[CH2:7]1)[C:3]([NH:22][C:23]1[CH:24]=[CH:25][C:26]([C:29]2[NH:33][C:32](=[O:34])[O:31][N:30]=2)=[CH:27][CH:28]=1)=[O:5]
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참가 물질

5

반응물 4

HCID 120603-Iodobenzoic acidHCID 27583524,4-DifluoropiperidineHCID 672227922-Hydroxy-2-[4-(p-tolylsulfonyl)morpholin-2-yl]acetic acidHCID 178507458HCID 178507458, 화합물

생성물 1

HCID 1363377932-hydroxy-N-[4-(5-oxo-4H-1,2,4-oxadiazol-3-yl)phenyl]-2-[4-(p-tolylsulfonyl)morpholin-2-yl]acetamide수율 58.7%

실험 절차

According to the Step 77-1 in synthetic method for EXAMPLE 77, compound 116-2 (94 mg) and 3-(4-aminophenyl)-1,2,4-oxadiazol-5(2H)-one (79.2 mg) were used instead of 3-iodobenzoic acid and 4,4-difluoropiperidine to obtain compound 116-3 (83 mg) as a pale yellow amorphous solid.

출처 및 근거

ORD 기록
ord-1c986cbfb749497abde96fc05a446243
출처 데이터셋
uspto-grants-2015_03
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08987242B2

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