Triethylamine → HCID 131724455、化合物

HRID 352246

反応式

HRID 352246 の反応式
N[CH:2]1[CH2:6][CH2:5][CH:4]([N:7]2[C:16]3[CH:15]=[CH:14][CH:13]=[C:12]([Cl:17])[C:11]=3[C:10]3=[N:18][O:19][C:20]([CH3:21])=[C:9]3[C:8]2=[O:22])[CH2:3]1.[CH3:23][O:24][C:25]1[CH:26]=[C:27]([CH2:35][C:36]([OH:38])=O)[CH:28]=[C:29]([O:33][CH3:34])[C:30]=1[O:31][CH3:32].CC[N:41](CC)CC.C1C=CC2N(O)N=NC=2C=1.CCN=C=NCCCN(C)C>C(Cl)Cl.CN(C1C=CN=CC=1)C>[Cl:17][C:12]1[C:11]2[C:10]3[C:9](=[C:20]([CH3:21])[O:19][N:18]=3)[C:8](=[O:22])[N:7]([C:4]3([C:29]4([O:33][CH3:34])[C:30]([O:31][CH3:32])=[C:25]([O:24][CH3:23])[CH:26]=[C:27]([CH2:35][C:36]([NH2:41])=[O:38])[CH2:28]4)[CH2:3][CH2:2][CH2:6][CH2:5]3)[C:16]=2[CH:15]=[CH:14][CH:13]=1

参加物

8

反応物 5

HCID 8471TriethylamineHCID 159081-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 703723,4,5-Trimethoxyphenylacetic acidHCID 757711-HydroxybenzotriazoleHCID 22713955HCID 22713955、化合物

生成物 1

HCID 131724455HCID 131724455、化合物収率 66%

試薬・触媒・溶媒 2

HCID 142844-(Dimethylamino)pyridine触媒HCID 6344Dichloromethane溶媒2 回

実験手順

To a stirred solution of racemic 5-(3-aminocyclopentyl)-9-chloro-3-methyl-5H-isoxazolo[4,3-c]quinolin-4-one (81 mg, 0.26 mmol) in CH2Cl2 (3 mL) was added 3,4,5-trimethoxy phenyl acetic acid (114 mg, 0.52 mmol), Et3N (0.1 mL, 0.50 mmol), HOBt (41 mg, 0.3 mmol),DMAP (catalytic amount) and EDCI (72 mg, 0.38 mmol). The reaction mixture was stirred at r.t. for 18 hours. The mixture was diluted with CH2Cl2, washed (brine), dried (Na2SO4), filtered and concentrated. Column chromatography (silica gel, hexanes/ethyl acetate, gradient) gave the racemic title compound (89 mg, 66%). Mass Spectrum (FIA) (m/z) 454.0 (M+1)

後処理

  1. washwashed (brine)
  2. dry with materialdried (Na2SO4)
  3. filtrationfiltered
  4. concentrationconcentrated

出典と根拠

ORDレコード
ord-3f64bbca03c94c9d838d6d8d06135089
出典データセット
uspto-grants-2004_06
特許番号
US06743794B2

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