3-碘吡啶 → (S)-2-morpholin-4-yl-9-pyridin-3-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one

HRID 80611

反应方程式

HRID 80611 反应方程式
[N:1]1([C:7]2[N:8]=[C:9]3[NH:17][C@H:16]([C:18]([F:21])([F:20])[F:19])[CH2:15][CH2:14][N:10]3[C:11](=[O:13])[CH:12]=2)[CH2:6][CH2:5][O:4][CH2:3][CH2:2]1.I[C:23]1[CH:24]=[N:25][CH:26]=[CH:27][CH:28]=1>>[N:1]1([C:7]2[N:8]=[C:9]3[N:17]([C:23]4[CH:24]=[N:25][CH:26]=[CH:27][CH:28]=4)[C@H:16]([C:18]([F:20])([F:21])[F:19])[CH2:15][CH2:14][N:10]3[C:11](=[O:13])[CH:12]=2)[CH2:6][CH2:5][O:4][CH2:3][CH2:2]1

参与物

3

反应物 2

HCID 707143-碘吡啶HCID 136238743(S)-8-(Morpholin-4-yl)-2-(trifluoromethyl)-1,2,3,4-tetrahydropyrimido[1,2-a]pyrimidin-6-one

产物 1

HCID 49854091(S)-2-morpholin-4-yl-9-pyridin-3-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one

实验过程

The product is prepared according to the procedure described in Example 12, using 200 mg of (S)-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one (Example 1e) and 380 mg of 3-iodopyridine. After purification by silica chromatography (elution gradient of CH2Cl2 to CH2Cl2/MeOH 96/04), 48 mg of (S)-2-morpholin-4-yl-9-pyridin-3-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one are obtained, in the form of a yellow solid, the characteristics of which are the following:

后处理

  1. customThe product is prepared
  2. customAfter purification
  3. washby silica chromatography (elution gradient of CH2Cl2 to CH2Cl2/MeOH 96/04), 48 mg of (S)-2-morpholin-4-yl-9-pyridin-3-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one
  4. customare obtained, in the form of a yellow solid

来源与证据

ORD记录
ord-5120b98da0ed46d6bd4614ae9b81f0c5
来源数据集
uspto-grants-2014_09
专利号
US08846670B2

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