Trifluoroacetic acid → 7-amino-4-(3,4-dihydroxycyclopentyl)-2-methyl-2,3-dihydro-1H-isoindol-1-one trifluoroacetate

HRID 511489ノート

反応式

HRID 511489 の反応式
[OH:1][CH:2]1[CH:6]([OH:7])[CH2:5][CH:4]([C:8]2[CH:9]=[CH:10][C:11]([NH:19]C(=O)OC(C)(C)C)=[C:12]3[C:16]=2[CH2:15][N:14]([CH3:17])[C:13]3=[O:18])[CH2:3]1.[C:27]([OH:33])([C:29]([F:32])([F:31])[F:30])=[O:28]>C(Cl)Cl>[F:30][C:29]([F:32])([F:31])[C:27]([OH:33])=[O:28].[NH2:19][C:11]1[CH:10]=[CH:9][C:8]([CH:4]2[CH2:3][CH:2]([OH:1])[CH:6]([OH:7])[CH2:5]2)=[C:16]2[C:12]=1[C:13](=[O:18])[N:14]([CH3:17])[CH2:15]2

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 86695307tert-butyl[7-(3,4-dihydroxycyclopentyl)-2-methyl-3-oxo-2,3-dihydro-1H-isoindol-4-yl]carbamate2 回

生成物 1

HCID 672550847-amino-4-(3,4-dihydroxycyclopentyl)-2-methyl-2,3-dihydro-1H-isoindol-1-one trifluoroacetate

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

To a solution of tert-butyl [7-(3,4-dihydroxycyclopentyl)-2-methyl-3-oxo-2,3-dihydro-1H-isoindol-4-yl]carbamate (Compound 243B, 36 mg, 0.099 mmol) in DCM (2 mL) was added TFA (1 mL). The resulting mixture was stirred at rt for 30 min, then evaporated under reduced pressure to give the desired product. This TFA salt was directly used in next step. MS (ES+): m/z=263.09 [MH+]. HPLC: tR=0.78 min (ZQ3, polar—5 min).

後処理

  1. customevaporated under reduced pressure

出典と根拠

ORDレコード
ord-b8c0fececcb94206a2c40835b157621b
出典データセット
uspto-grants-2015_08
特許番号
US09096624B2

反応ノート

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