Hydrochloric Acid → (3R)-3-(cyclopentylmethyl)-4-(5-{[(5-fluoro-2-pyridinyl)amino]carbonyl}-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoic acid

HRID 1396975ノート

反応式

HRID 1396975 の反応式
[CH:1]1([CH2:6][C@@H:7]([C:16]([N:18]2[CH:22]([C:23]([NH:25][C:26]3[CH:31]=[CH:30][C:29]([F:32])=[CH:28][N:27]=3)=[O:24])[CH2:21][CH:20]=[N:19]2)=[O:17])[CH2:8][C:9]([O:11]C(C)(C)C)=[O:10])[CH2:5][CH2:4][CH2:3][CH2:2]1.Cl>O1CCOCC1>[CH:1]1([CH2:6][C@@H:7]([C:16]([N:18]2[CH:22]([C:23]([NH:25][C:26]3[CH:31]=[CH:30][C:29]([F:32])=[CH:28][N:27]=3)=[O:24])[CH2:21][CH:20]=[N:19]2)=[O:17])[CH2:8][C:9]([OH:11])=[O:10])[CH2:5][CH2:4][CH2:3][CH2:2]1

参加物

4

反応物 2

HCID 313Hydrochloric AcidHCID 682881271,1-dimethylethyl (3R)-3-(cyclopentylmethyl)-4-(5-{[(5-fluoro-2-pyridinyl)amino]carbonyl}-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoate

生成物 1

HCID 68287946(3R)-3-(cyclopentylmethyl)-4-(5-{[(5-fluoro-2-pyridinyl)amino]carbonyl}-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoic acid収率 100.7%

試薬・触媒・溶媒 1

HCID 312751,4-Dioxane溶媒2 回

実験手順

To a solution of 1,1-dimethylethyl (3R)-3-(cyclopentylmethyl)-4-(5-{[(5-fluoro-2-pyridinyl)amino]carbonyl}-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoate (323 mg, 0.72 mmol) in 1,4-dioxane (5.0 mL) was added 4.0 M hydrochloric acid in 1,4-dioxane (9.0 mL, 36 mmol) at room temperature. The reaction mixture was stirred for 4 hours. After this time, the solvent was removed by reduced pressure to afford the crude product, (3R)-3-(cyclopentylmethyl)-4-(5-{[(5-fluoro-2-pyridinyl)amino]carbonyl}-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoic acid (283 mg, 100%), which was used directly in the next step. MS: 491 ([M+H]+).

後処理

  1. customAfter this time, the solvent was removed by reduced pressure

出典と根拠

ORDレコード
ord-b489069eee1442fcbbd359b23d24595d
出典データセット
uspto-grants-2014_12
特許番号
US08901119B2

反応ノート

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