Lithium Hydroxide → HCID 86728307, 화합물

HRID 1776929노트

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HRID 1776929 반응식
[F:1][C:2]1[C:3]2[C:4]([CH:45]([OH:51])[C:46]([O:48]CC)=[O:47])=[C:5]3[C:14]4[N:15]=[C:16]([C:19]5[C:20]([N:39]([CH3:44])[S:40]([CH3:43])(=[O:42])=[O:41])=[CH:21][C:22]6[O:26][C:25]([C:27]7[CH:32]=[CH:31][C:30]([F:33])=[CH:29][CH:28]=7)=[C:24]([C:34](=[O:37])[NH:35][CH3:36])[C:23]=6[CH:38]=5)[CH:17]=[CH:18][C:13]=4[O:12][CH2:11][N:6]3[C:7]=2[CH:8]=[CH:9][CH:10]=1.[OH-].[Li+]>C1COCC1.O.CO>[F:1][C:2]1[C:3]2[C:4]([CH:45]([OH:51])[C:46]([OH:48])=[O:47])=[C:5]3[C:14]4[N:15]=[C:16]([C:19]5[C:20]([N:39]([CH3:44])[S:40]([CH3:43])(=[O:42])=[O:41])=[CH:21][C:22]6[O:26][C:25]([C:27]7[CH:28]=[CH:29][C:30]([F:33])=[CH:31][CH:32]=7)=[C:24]([C:34](=[O:37])[NH:35][CH3:36])[C:23]=6[CH:38]=5)[CH:17]=[CH:18][C:13]=4[O:12][CH2:11][N:6]3[C:7]=2[CH:8]=[CH:9][CH:10]=1

참가 물질

6

반응물 2

HCID 3939Lithium HydroxideHCID 86728306HCID 86728306, 화합물

생성물 1

HCID 86728307HCID 86728307, 화합물

시약·촉매·용매 3

HCID 887Methanol용매HCID 962Water용매HCID 8028Tetrahydrofuran용매

실험 절차

A mixture of ethyl 2-(11-fluoro-2-(2-(4-fluorophenyl)-3-(methylcarbamoyl)-6-(N-methylmethylsulfonamido)benzofuran-5-yl)-6H-pyrido[2′,3′:5,6][1,3]oxazino[3,4-a]indol-12-yl)-2-hydroxyacetate (233 mg, 0.325 mmol) and lithium hydroxide (54.5 mg, 2.276 mmol) in THF (1 ml), water (0.5 ml) and MeOH (0.5 ml) was stirred at room temperature over night, then concentrated under vacuum. The resulting residue was purified using EP column (30 mm×250 mm), 60% IPA/CO2. This resulted in 128 mg (57.2%) of 2-(11-fluoro-2-(2-(4-fluorophenyl) -3-(methylcarbamoyl)-6-(N-methylmethylsulfonamido)benzofuran-5-yl)-6H-pyrido[2′,3′:5,6][1,3]oxazino[3,4-a]indol-12-yl)-2-hydroxyacetic acid (Compound 207) as a white solid. LC-MS (ES, m/z) C34H26F2N4O8S: 688. Found: 689 [M+H]+.

후처리

  1. concentrationconcentrated under vacuum
  2. customThe resulting residue was purified

출처 및 근거

ORD 기록
ord-1c6374b4ec3342d7ac1012d63de8e280
출처 데이터셋
uspto-grants-2016_02
특허 번호
US09265773B2

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