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

HRID 1678501ノート

反応式

HRID 1678501 の反応式
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]

参加物

8

反応物 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

生成物 1

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

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

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)

後処理

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

出典と根拠

ORDレコード
ord-ea056892380d44d4bf87895aaf8d113c
出典データセット
uspto-grants-2011_08
特許番号
US08008303B2

反応ノート

読み込み中…