Ammonia dioxane → N-{1-[5-(Aminosulfonyl)-1,3-thiazol-2-yl]piperidin-4-yl}-3,4-dichloro-5-methyl-1H-pyrrole-2-carboxamide

HRID 2234018노트

반응식

HRID 2234018 반응식
[NH3:1].O1CCOCC1.[Cl:8][C:9]1[C:13]([Cl:14])=[C:12]([CH3:15])[NH:11][C:10]=1[C:16]([NH:18][CH:19]1[CH2:24][CH2:23][N:22]([C:25]2[S:26][C:27]([S:30]([OH:33])(=O)=[O:31])=[CH:28][N:29]=2)[CH2:21][CH2:20]1)=[O:17]>>[NH2:1][S:30]([C:27]1[S:26][C:25]([N:22]2[CH2:23][CH2:24][CH:19]([NH:18][C:16]([C:10]3[NH:11][C:12]([CH3:15])=[C:13]([Cl:14])[C:9]=3[Cl:8])=[O:17])[CH2:20][CH2:21]2)=[N:29][CH:28]=1)(=[O:33])=[O:31]

참가 물질

3

반응물 2

HCID 66648793Ammonia dioxaneHCID 866083382-(4-{[(3,4-Dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-1,3-thiazole-5-sulfonic acid

생성물 1

HCID 68580500N-{1-[5-(Aminosulfonyl)-1,3-thiazol-2-yl]piperidin-4-yl}-3,4-dichloro-5-methyl-1H-pyrrole-2-carboxamide수율 56.5%

실험 절차

0.5 M ammonia/dioxane (10 ml, 5 mmol) was added to 2-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-1,3-thiazole-5-sulfonic acid (Example 254; 100 mg, 0.226 mmol) in a pressure bottle. The mixture was stirred at room temperature for 4 h. Excess solvent was removed in vacuo and the brown solid was dried in vacuo to give the title compound (56 mg).

후처리

  1. customExcess solvent was removed in vacuo
  2. customthe brown solid was dried in vacuo

출처 및 근거

ORD 기록
ord-23a33f93735e4a5aa0b7835d5f45fe8b
출처 데이터셋
uspto-grants-2010_05
특허 번호
US07709503B2

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