Triethylamine → 8-Chloro-7-{4-[(cyclohexylamino)carbonyl]piperidin-1-yl}-1-cyclopropyl-n-(2,4-dichlorobenzyl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide

HRID 1011224

반응식

HRID 1011224 반응식
[Cl:1][C:2]1[C:3](F)=[C:4]([F:28])[CH:5]=[C:6]2[C:11]=1[N:10]([CH:12]1[CH2:14][CH2:13]1)[CH:9]=[C:8]([C:15]([NH:17][CH2:18][C:19]1[CH:24]=[CH:23][C:22]([Cl:25])=[CH:21][C:20]=1[Cl:26])=[O:16])[C:7]2=[O:27].[CH:30]1([NH:36][C:37]([CH:39]2[CH2:44][CH2:43][NH:42][CH2:41][CH2:40]2)=[O:38])[CH2:35][CH2:34][CH2:33][CH2:32][CH2:31]1.C(N(CC)CC)C>CS(C)=O>[Cl:1][C:2]1[C:3]([N:42]2[CH2:43][CH2:44][CH:39]([C:37]([NH:36][CH:30]3[CH2:31][CH2:32][CH2:33][CH2:34][CH2:35]3)=[O:38])[CH2:40][CH2:41]2)=[C:4]([F:28])[CH:5]=[C:6]2[C:11]=1[N:10]([CH:12]1[CH2:14][CH2:13]1)[CH:9]=[C:8]([C:15]([NH:17][CH2:18][C:19]1[CH:24]=[CH:23][C:22]([Cl:25])=[CH:21][C:20]=1[Cl:26])=[O:16])[C:7]2=[O:27]

참가 물질

5

반응물 3

HCID 8471TriethylamineHCID 12410238HCID 12410238, 화합물HCID 577809783-Quinolinecarboxamide,8-chloro-1-cyclopropyl-n-[(2,4-dichlorophenyl)methyl]-6,7-difluoro-1,4-dihydro-4-oxo-

생성물 1

HCID 577809288-Chloro-7-{4-[(cyclohexylamino)carbonyl]piperidin-1-yl}-1-cyclopropyl-n-(2,4-dichlorobenzyl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide수율 10.5%

시약·촉매·용매 1

HCID 679Dimethyl Sulfoxide용매

실험 절차

200 mg (0.44 mmol) of the compound of Example 70A and 138 mg (0.66 mmol) of 4-(cyclohexylamino)carbonylpiperidine (for preparation see WO 2003031397) are heated with 91 μl (0.66 mmol) of triethylamine in 4 ml of DMSO at 120° C. for 7 h. After cooling, the entire reaction mixture is separated by preparative HPLC (method 6). 30 mg of the title compound are obtained.

후처리

  1. temperatureAfter cooling
  2. customthe entire reaction mixture
  3. customis separated by preparative HPLC (method 6)

출처 및 근거

ORD 기록
ord-b42459cec24e4bdf830f1a3db0db7fd8
출처 데이터셋
uspto-grants-2011_07
특허 번호
US07977349B2

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