Water → {4'-[4-(4-Dimethylsulfamoyl-piperazin-1-ylmethyl)-phenylcarbamoyl]-6-trifluoromethoxy-biphenyl-3-yl}-carboxylic acid tert-butyl ester

HRID 1678501노트

반응식

HRID 1678501 반응식
C(OC(N[C:9]1[CH:10]=[CH:11][C:12]([O:24][C:25]([F:28])([F:27])[F:26])=[C:13]([C:15]2[CH:20]=[CH:19][C:18]([C:21]([OH:23])=O)=[CH:17][CH:16]=2)[CH:14]=1)=O)(C)(C)C.[CH3:29][N:30]([CH3:48])[S:31]([N:34]1[CH2:39][CH2:38][N:37]([CH2:40][C:41]2[CH:46]=[CH:45][C:44]([NH2:47])=[CH:43][CH:42]=2)[CH2:36][CH2:35]1)(=[O:33])=[O:32].CCN=C=N[CH2:54][CH2:55][CH2:56]N(C)C.[CH:60]1C=CC2N(O)N=NC=2C=1.CN1CC[O:74][CH2:73]C1.[OH2:77]>CN(C=O)C>[C:55]([O:77][C:73]([C:9]1[CH:14]=[C:13]([C:15]2[CH:20]=[CH:19][C:18]([C:21](=[O:23])[NH:47][C:44]3[CH:45]=[CH:46][C:41]([CH2:40][N:37]4[CH2:36][CH2:35][N:34]([S:31](=[O:32])(=[O:33])[N:30]([CH3:48])[CH3:29])[CH2:39][CH2:38]4)=[CH:42][CH:43]=3)=[CH:17][CH:16]=2)[C:12]([O:24][C:25]([F:27])([F:28])[F:26])=[CH:11][CH:10]=1)=[O:74])([CH3:56])([CH3:60])[CH3:54]

참가 물질

8

반응물 6

HCID 962WaterHCID 79724-MethylmorpholineHCID 159081-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 757711-HydroxybenzotriazoleHCID 282735524-(4-Amino-benzyl)-piperazine-1-sulfonic acid dimethylamideHCID 598223415'-tert-Butoxycarbonylamino-2'-trifluoromethoxy-biphenyl-4-carboxylic acid

생성물 1

HCID 67373671{4'-[4-(4-Dimethylsulfamoyl-piperazin-1-ylmethyl)-phenylcarbamoyl]-6-trifluoromethoxy-biphenyl-3-yl}-carboxylic acid tert-butyl ester

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

A mixture of 5′-tert-butoxycarbonylamino-2′-trifluoromethoxy-biphenyl-4-carboxylic acid (300 mg), 4-(4-amino-benzyl)-piperazine-1-sulfonic acid dimethylamide (226 mg), EDAC (144 mg) and HOBT (103 mg) in dry DMF (3 ml) containing N-methyl morpholine (0.166 ml) was stirred for 16 h. The mixture was then added to water (12 ml) and the resulting solid collected by filtration and dried and used in the following step without purification (558 mg)

후처리

  1. filtrationthe resulting solid collected by filtration
  2. customdried
  3. customused in the following step without purification (558 mg)

출처 및 근거

ORD 기록
ord-ea056892380d44d4bf87895aaf8d113c
출처 데이터셋
uspto-grants-2011_08
특허 번호
US08008303B2

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