Triethylamine → 3-[2-[N-(4-Fluoro-2-trifluoromethylphenyl)sulfamoyl]acetylamino]-3-carboxypropionic Acid Methyl Ester

HRID 248717ノート

反応式

HRID 248717 の反応式
[F:1][C:2]1[CH:7]=[CH:6][C:5]([NH:8][S:9]([CH2:12][C:13]([OH:15])=O)(=[O:11])=[O:10])=[C:4]([C:16]([F:19])([F:18])[F:17])[CH:3]=1.Cl.C[O:22][C:23](=[O:31])[C@H:24]([CH2:26][C:27]([O:29][CH3:30])=[O:28])[NH2:25].O.OC1C2N=NNC=2C=CC=1.C(N(CC)CC)C.C1(N=C=NC2CCCCC2)CCCCC1>>[CH3:30][O:29][C:27](=[O:28])[CH2:26][CH:24]([NH:25][C:13](=[O:15])[CH2:12][S:9](=[O:10])(=[O:11])[NH:8][C:5]1[CH:6]=[CH:7][C:2]([F:1])=[CH:3][C:4]=1[C:16]([F:19])([F:18])[F:17])[C:23]([OH:31])=[O:22]

参加物

6

反応物 5

HCID 8471TriethylamineHCID 10868DicyclohexylcarbodiimideHCID 2734892L-Aspartic acid, 1,4-dimethyl ester, hydrochloride (1:1)HCID 156765552-[N-(4-fluoro-2-trifluoromethylphenyl)sulfamoyl]acetic acidHCID 178526939HCID 178526939、化合物

生成物 1

HCID 540670863-[2-[N-(4-Fluoro-2-trifluoromethylphenyl)sulfamoyl]acetylamino]-3-carboxypropionic Acid Methyl Ester

実験手順

Under the conditions of Example 2(a), 3.012 g (10 mmol) of 2-[2-[N-(4-fluoro-2-trifluoromethylphenyl)sulfamoyl]acetic acid, 1.836 g (10 mmol) of L-aspartic acid dimethyl ester hydrochoride, 1,531 g (10 mmol) of hydroxybenzotriazole, hydrate, as well as 1.012 g (10 mmol) of triethylamine and 2.063 g (10 mmol) of dicyclohexylcarbodiimide are reacted and worked up analogously. The crude product is purified by column chromatography on silica gel. The title compound is eluted with ethyl acetate.

後処理

  1. customThe crude product is purified by column chromatography on silica gel
  2. washThe title compound is eluted with ethyl acetate

出典と根拠

ORDレコード
ord-45089767ebf64197a07bbfa6146b90be
出典データセット
uspto-grants-1993_05
特許番号
US05210290

反応ノート

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