Pyridine → (R)-3-((S)-1-(2-(2-Ethylphenoxy)phenyl)-1-hydroxy-5-methoxypentyl)piperidine-1-carbonyl Chloride

HRID 253593

反応式

HRID 253593 の反応式
[CH2:1]([C:3]1[CH:29]=[CH:28][CH:27]=[CH:26][C:4]=1[O:5][C:6]1[CH:11]=[CH:10][CH:9]=[CH:8][C:7]=1[C@:12]([C@@H:20]1[CH2:25][CH2:24][CH2:23][NH:22][CH2:21]1)([OH:19])[CH2:13][CH2:14][CH2:15][CH2:16][O:17][CH3:18])[CH3:2].N1C=CC=CC=1.[Cl:36][C:37](Cl)([O:39]C(=O)OC(Cl)(Cl)Cl)Cl>C(Cl)Cl>[CH2:1]([C:3]1[CH:29]=[CH:28][CH:27]=[CH:26][C:4]=1[O:5][C:6]1[CH:11]=[CH:10][CH:9]=[CH:8][C:7]=1[C@:12]([C@@H:20]1[CH2:25][CH2:24][CH2:23][N:22]([C:37]([Cl:36])=[O:39])[CH2:21]1)([OH:19])[CH2:13][CH2:14][CH2:15][CH2:16][O:17][CH3:18])[CH3:2]

参加物

5

反応物 3

HCID 1049PyridineHCID 94429TriphosgeneHCID 59383027(S)-1-(2-(2-ethylphenoxy)phenyl)-5-methoxy-1-((R)-piperidin-3-yl)pentan-1-ol

生成物 1

HCID 57786487(R)-3-((S)-1-(2-(2-Ethylphenoxy)phenyl)-1-hydroxy-5-methoxypentyl)piperidine-1-carbonyl Chloride

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒2 回

実験手順

To a solution of (S)-1-(2-(2-ethylphenoxy)phenyl)-5-methoxy-1-((R)-piperidin-3-yl)pentan-1-ol (19.9 mg, 0.05 mmol) and pyridine (20 μL, 0.15 mmol) in CH2Cl2 (2 mL) at 0° C. was added triphosgene (22.7 mg, 0.08 mmol) in CH2Cl2 (0.5 mL). The resulting solution was warmed to rt, and stirred for 1 h. The completion of reaction was confirmed by LC-MS, and the product was used for next step without workup.

後処理

  1. customThe completion of reaction

出典と根拠

ORDレコード
ord-5d19f2e425a44ae8a9dc7952d26b0674
出典データセット
uspto-grants-2011_01
特許番号
US07872028B2

関連ノート

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