Methanol → N-[3,5-Dichloro-4-(3-cyclopropylmethanesulfonyl-4-hydroxy-phenoxy)-phenyl]-malonamic acid ethyl ester

HRID 432930노트

반응식

HRID 432930 반응식
[NH2:1][C:2]1[CH:22]=[C:21]([Cl:23])[C:5]([O:6][C:7]2[CH:12]=[CH:11][C:10]([OH:13])=[C:9]([S:14]([CH2:17][CH:18]3[CH2:20][CH2:19]3)(=[O:16])=[O:15])[CH:8]=2)=[C:4]([Cl:24])[CH:3]=1.C(N([CH2:30][CH3:31])CC)C.C([CH:34]([C:38](Cl)=[O:39])[C:35](Cl)=[O:36])C.C[OH:42]>C1COCC1.C(Cl)Cl>[CH2:30]([O:42][C:38](=[O:39])[CH2:34][C:35]([NH:1][C:2]1[CH:3]=[C:4]([Cl:24])[C:5]([O:6][C:7]2[CH:12]=[CH:11][C:10]([OH:13])=[C:9]([S:14]([CH2:17][CH:18]3[CH2:20][CH2:19]3)(=[O:16])=[O:15])[CH:8]=2)=[C:21]([Cl:23])[CH:22]=1)=[O:36])[CH3:31]

참가 물질

7

반응물 4

HCID 887MethanolHCID 8471Triethylamine2회HCID 109209242-Ethylpropanedioyl dichlorideHCID 692599874-(4-Amino-2,6-dichloro-phenoxy)-2-cyclopropylmethanesulfonyl-phenol

생성물 1

HCID 69260451N-[3,5-Dichloro-4-(3-cyclopropylmethanesulfonyl-4-hydroxy-phenoxy)-phenyl]-malonamic acid ethyl ester

시약·촉매·용매 2

HCID 6344Dichloromethane용매HCID 8028Tetrahydrofuran용매2회

실험 절차

To a solution of 4-(4-amino-2,6-dichloro-phenoxy)-2-cyclopropylmethane-sulfonyl-phenol (43 mg, 0.11 mmol) in THF (2 mL) was added triethylamine (17 μL, 0.12 mmol) in THF (2 mL) was added triethylamine (17 μL, 0.12 mmol) and ethyl malonyl chloride (14 μL, 0.11 mmol). The resulting mixture was preparative TLC (2% MeOH in CH2Cl2) to give the title compound of Step F (42 mg). MS (APCl−) Calc.: 501.0, Found: 500.3 (M−1).

출처 및 근거

ORD 기록
ord-883173b6f16740beaf5187152b5abe88
출처 데이터셋
uspto-grants-2003_12
특허 번호
US06664291B2

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