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 489793노트

반응식

HRID 489793 반응식
[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]

참가 물질

3

반응물 1

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

생성물 1

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

시약·촉매·용매 1

HCID 313Hydrochloric Acid용매

실험 절차

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.

후처리

  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

출처 및 근거

ORD 기록
ord-0546cc285e0442d887080458a432d28b
출처 데이터셋
uspto-grants-2005_12
특허 번호
US06979690B2

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