N-(4-(3-(3,4-dihydro-2H-pyran-2-yl)pyridin-2-yloxy)phenyl)benzo[d]thiazol-2-amine → (+/-)-N-(4-(3-(Tetrahydro-2H-pyran-2-YL)pyridin-2-yloxy)phenyl)benzo[D]thiazol-2-amine

HRID 1880100ノート

反応式

HRID 1880100 の反応式
[O:1]1[CH:6]=[CH:5][CH2:4][CH2:3][CH:2]1[C:7]1[C:8]([O:13][C:14]2[CH:19]=[CH:18][C:17]([NH:20][C:21]3[S:22][C:23]4[CH:29]=[CH:28][CH:27]=[CH:26][C:24]=4[N:25]=3)=[CH:16][CH:15]=2)=[N:9][CH:10]=[CH:11][CH:12]=1>[Pd].C(O)C>[O:1]1[CH2:6][CH2:5][CH2:4][CH2:3][CH:2]1[C:7]1[C:8]([O:13][C:14]2[CH:19]=[CH:18][C:17]([NH:20][C:21]3[S:22][C:23]4[CH:29]=[CH:28][CH:27]=[CH:26][C:24]=4[N:25]=3)=[CH:16][CH:15]=2)=[N:9][CH:10]=[CH:11][CH:12]=1

参加物

4

反応物 1

HCID 59326996N-(4-(3-(3,4-dihydro-2H-pyran-2-yl)pyridin-2-yloxy)phenyl)benzo[d]thiazol-2-amine

生成物 1

HCID 59326804(+/-)-N-(4-(3-(Tetrahydro-2H-pyran-2-YL)pyridin-2-yloxy)phenyl)benzo[D]thiazol-2-amine

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 702Ethanol溶媒

実験手順

A mixture of N-(4-(3-(3,4-dihydro-2H-pyran-2-yl)pyridin-2-yloxy)phenyl)benzo[d]thiazol-2-amine (357 mg, 0.889 mmol) and palladium on carbon, wet (95 mg, 0.089 mmol) in ethanol (0.15M) was placed under an atmosphere of hydrogen (g) and stirred at room temperature. After the starting material was completely consumed, the mixture was filtered through a cake of celite, washed with MeOH & THF and filtrate was concentrated to dryness. The residue was purified by silica gel chromatography to give the desired product as a racemic mixture. MS (ESI, pos. ion) m/z: 404.0 (M+1). IC50 (uM) +++++.

後処理

  1. customAfter the starting material was completely consumed
  2. filtrationthe mixture was filtered through a cake of celite
  3. washwashed with MeOH & THF and filtrate
  4. concentrationwas concentrated to dryness
  5. customThe residue was purified by silica gel chromatography

出典と根拠

ORDレコード
ord-c486b186c57e4e1bb5d78b9e393a03e1
出典データセット
uspto-grants-2012_11
特許番号
US08318718B2

反応ノート

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