Sodium Carbonate → [5-(2-Methoxy-5-trifluoromethyl-phenyl)-3-methyl-pyridin-2-yl]-(4-pyrrolidin-1-yl-piperidin-1-yl)-methanone

HRID 1517099

反応式

HRID 1517099 の反応式
COC(C1C(C)=CC(C2C=CC=C(C(F)(F)F)C=2)=CN=1)=O.ClC1C=C([C:30]2[CH:31]=[C:32]([CH3:49])[C:33]([C:36]([N:38]3[CH2:43][CH2:42][CH:41]([N:44]4[CH2:48][CH2:47][CH2:46][CH2:45]4)[CH2:40][CH2:39]3)=[O:37])=[N:34][CH:35]=2)C=CC=1Cl.[CH3:50][O:51][C:52]1[CH:57]=[CH:56][C:55]([C:58]([F:61])([F:60])[F:59])=[CH:54][C:53]=1B(O)O.C(=O)([O-])[O-].[Na+].[Na+]>O1CCOCC1.O.[Pd](Cl)Cl>[CH3:50][O:51][C:52]1[CH:57]=[CH:56][C:55]([C:58]([F:61])([F:60])[F:59])=[CH:54][C:53]=1[C:30]1[CH:31]=[C:32]([CH3:49])[C:33]([C:36]([N:38]2[CH2:39][CH2:40][CH:41]([N:44]3[CH2:48][CH2:47][CH2:46][CH2:45]3)[CH2:42][CH2:43]2)=[O:37])=[N:34][CH:35]=1

参加物

7

反応物 4

HCID 10340Sodium CarbonateHCID 27826762-Methoxy-5-(trifluoromethyl)phenylboronic acidHCID 574411233-Methyl-5-(3-trifluoromethyl-phenyl)-pyridine-2-carboxylic acid methyl esterHCID 58016731[5-(3,4-Dichloro-phenyl)-3-methyl-pyridin-2-yl]-(4-pyrrolidin-1-yl-piperidin-1-yl)-methanone

生成物 1

HCID 44547503[5-(2-Methoxy-5-trifluoromethyl-phenyl)-3-methyl-pyridin-2-yl]-(4-pyrrolidin-1-yl-piperidin-1-yl)-methanone

試薬・触媒・溶媒 2

HCID 24290Palladium Chloride触媒HCID 218864351,4-Dioxane--water (1/1)溶媒

実験手順

In analogy to the procedure described for the preparation of intermediate 1A, (5-bromo-3-methyl-pyridin-2-yl)-(4-pyrrolidin-1-yl-piperidin-1-yl)-methanone (see example 28) was reacted with 2-methoxy-5-trifluoromethyl-phenyl-boronic acid, (1,1′-bis-diphenylphosphino)-ferrocene)palladium-(II)dichloride (1:1 complex with CH2Cl2) and sodium carbonate in dioxane/water to give the title compound as brown amorphous solid. MS: 448.1 (MH+).

出典と根拠

ORDレコード
ord-c61d73ee54344a778a7e10a9aca99606
出典データセット
uspto-grants-2012_07
特許番号
US08227613B2

関連ノート

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