Tert-butyl 4-{3-[6-amino-5-chloro-2-(methyloxy)-3-pyridinyl]-3-oxopropyl}-1-piperidinecarboxylate → 1-(6-Amino-5-chloro-2-methoxy-3-pyridinyl)-3-(4-piperidinyl)-1-propanone

HRID 489793ノート

反応式

HRID 489793 の反応式
[NH2:1][C:2]1[N:7]=[C:6]([O:8][CH3:9])[C:5]([C:10](=[O:26])[CH2:11][CH2:12][CH:13]2[CH2:18][CH2:17][N:16](C(OC(C)(C)C)=O)[CH2:15][CH2:14]2)=[CH:4][C:3]=1[Cl:27]>Cl>[NH2:1][C:2]1[N:7]=[C:6]([O:8][CH3:9])[C:5]([C:10](=[O:26])[CH2:11][CH2:12][CH:13]2[CH2:18][CH2:17][NH:16][CH2:15][CH2:14]2)=[CH:4][C:3]=1[Cl:27]

参加物

3

反応物 1

HCID 22262604Tert-butyl 4-{3-[6-amino-5-chloro-2-(methyloxy)-3-pyridinyl]-3-oxopropyl}-1-piperidinecarboxylate

生成物 1

HCID 222625871-(6-Amino-5-chloro-2-methoxy-3-pyridinyl)-3-(4-piperidinyl)-1-propanone収率 87%

試薬・触媒・溶媒 1

HCID 313Hydrochloric Acid溶媒

実験手順

A mixture of 1,1-dimethylethyl 4-{3-[6-amino-5-chloro-2-(methyloxy)-3-pyridinyl]-3-oxopropyl}-1-piperidinecarboxylate (step 4, 180 mg, 0.452 mmol) in 10% methanolic hydrochloric acid (2 ml) was stirred at room temperature for 18 h. After concentrated in vacuo, the mixture was dissolved in ethyl acetate (50 ml), washed with 2N aqueous sodium hydroxide (3 ml) and brine (5 ml), and dried over potassium carbonate. Removal of solvent gave 117.1 mg (87%) of the title compound as a white solid.

後処理

  1. concentrationAfter concentrated in vacuo
  2. dissolutionthe mixture was dissolved in ethyl acetate (50 ml)
  3. washwashed with 2N aqueous sodium hydroxide (3 ml) and brine (5 ml)
  4. dry with materialdried over potassium carbonate
  5. customRemoval of solvent

出典と根拠

ORDレコード
ord-0546cc285e0442d887080458a432d28b
出典データセット
uspto-grants-2005_12
特許番号
US06979690B2

反応ノート

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