Diisopropylethylamine → (S)-N-(1-{4-[1-(6-Chloro-2-pyrrolidin-1-yl-pyrimidin-4-yl)-piperidin-4-yl]-phenyl}-ethyl)acetamide

HRID 1470748ノート

反応式

HRID 1470748 の反応式
Cl[C:2]1[CH:7]=[C:6]([Cl:8])[N:5]=[C:4]([N:9]2[CH2:13][CH2:12][CH2:11][CH2:10]2)[N:3]=1.CCN(C(C)C)C(C)C.[NH:23]1[CH2:28][CH2:27][CH:26]([C:29]2[CH:34]=[CH:33][C:32]([C@@H:35]([NH:37][C:38](=[O:40])[CH3:39])[CH3:36])=[CH:31][CH:30]=2)[CH2:25][CH2:24]1>C1COCC1>[Cl:8][C:6]1[N:5]=[C:4]([N:9]2[CH2:13][CH2:12][CH2:11][CH2:10]2)[N:3]=[C:2]([N:23]2[CH2:28][CH2:27][CH:26]([C:29]3[CH:34]=[CH:33][C:32]([C@@H:35]([NH:37][C:38](=[O:40])[CH3:39])[CH3:36])=[CH:31][CH:30]=3)[CH2:25][CH2:24]2)[CH:7]=1

参加物

5

反応物 3

HCID 81531DiisopropylethylamineHCID 193535534,6-Dichloro-2-(pyrrolidin-1-yl)pyrimidineHCID 67125412(S)-N-[1-(4-piperidin-4-yl-phenyl)ethyl]-acetamide

生成物 1

HCID 86666705(S)-N-(1-{4-[1-(6-Chloro-2-pyrrolidin-1-yl-pyrimidin-4-yl)-piperidin-4-yl]-phenyl}-ethyl)acetamide

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒

実験手順

To 22 mg (0.1 mmol) 4,6-dichloro-2-pyrrolidin-1-yl-pyrimidine in 1 mL THF are added 17 μL (0.1 mol) DIPEA and 25 mg (0.1 mmol) (S)—N-[1-(4-piperidin-4-yl-phenyl)ethyl]-acetamide (V.1). The mixture is stirred at rt over night. The solvent is removed in vacuo and the residue is purified using reversed phase HPLC (eluent A: water+0.1% TFA, eluent B: MeOH) to yield the desired product.

後処理

  1. customThe solvent is removed in vacuo
  2. customthe residue is purified

出典と根拠

ORDレコード
ord-d964d0db31ff41438675d8992344c6a7
出典データセット
uspto-grants-2015_04
特許番号
US09006450B2

反応ノート

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