1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → N-Cyclopropyl-4-methoxy-2,6-dimethyl-N-({4-[(4-pyridin-3-ylpiperazin-1-yl)carbonyl]-1,3-oxazol-2-yl}methyl)benzenesulfonamide

HRID 469076

反応式

HRID 469076 の反応式
[CH:1]1([N:4]([CH2:18][C:19]2[O:20][CH:21]=[C:22]([C:24]([OH:26])=O)[N:23]=2)[S:5]([C:8]2[C:13]([CH3:14])=[CH:12][C:11]([O:15][CH3:16])=[CH:10][C:9]=2[CH3:17])(=[O:7])=[O:6])[CH2:3][CH2:2]1.CCN=C=NCCCN(C)C.C1C=C2N=NN(O)C2=CC=1.O.CCN(C(C)C)C(C)C.[N:58]1[CH:63]=[CH:62][CH:61]=[C:60]([N:64]2[CH2:69][CH2:68][NH:67][CH2:66][CH2:65]2)[CH:59]=1>CN(C=O)C>[CH:1]1([N:4]([CH2:18][C:19]2[O:20][CH:21]=[C:22]([C:24]([N:67]3[CH2:68][CH2:69][N:64]([C:60]4[CH:59]=[N:58][CH:63]=[CH:62][CH:61]=4)[CH2:65][CH2:66]3)=[O:26])[N:23]=2)[S:5]([C:8]2[C:13]([CH3:14])=[CH:12][C:11]([O:15][CH3:16])=[CH:10][C:9]=2[CH3:17])(=[O:6])=[O:7])[CH2:2][CH2:3]1

参加物

7

反応物 5

HCID 159081-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 81531DiisopropylethylamineHCID 4372341-(Pyridin-3-yl)piperazineHCID 27960291-Hydroxybenzotriazole hydrateHCID 583930982-({Cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)-1,3-oxazole-4-carboxylic acid

生成物 1

HCID 58393276N-Cyclopropyl-4-methoxy-2,6-dimethyl-N-({4-[(4-pyridin-3-ylpiperazin-1-yl)carbonyl]-1,3-oxazol-2-yl}methyl)benzenesulfonamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

The title compound was prepared according to general procedure AH using 2-({cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)-1,3-oxazole-4-carboxylic acid (50 mg, 0.13 mmol), EDCI (50 mg, 0.26 mmol), HOBt monohydrate (40 mg, 0.26 mmol), DIPEA (90 μL, 0.52 mmol), 1-pyridin-3-ylpiperazine (21 mg, 0.13 mmol) and DMF (1 mL). The resulting crude compound was purified by FCC eluting with 99:1 DCM:7N NH3 in MeOH.

後処理

  1. customThe resulting crude compound was purified by FCC
  2. washeluting with 99:1 DCM

出典と根拠

ORDレコード
ord-cd2762729c1b439cb88ea8116e06c5dd
出典データセット
uspto-grants-2014_01
特許番号
US08623859B2

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