(4-Bromo-2,6-dimethyl-phenyl)-[4-((S)-2-hydroxymethyl-pyrrolidin-1-yl)-piperidin-1-yl]-methanone → [4,6-Dimethyl-2-(3-trifluoromethyl-phenyl)-pyrimidin-5-yl]-(4-hydroxy-[1,4']bipiperidinyl-1'-yl)-methanone

HRID 1692416

反応式

HRID 1692416 の反応式
BrC1C=C(C)C(C(N2CCC(N3CCCC3)CC2)=O)=C(C)C=1.BrC1C=C(C)C(C(N2CCC(N3CCC[C@H]3CO)CC2)=O)=C(C)C=1.[CH3:47][C:48]1[C:53]([C:54]([OH:56])=O)=[C:52]([CH3:57])[N:51]=[C:50]([C:58]2[CH:63]=[CH:62][CH:61]=[C:60]([C:64]([F:67])([F:66])[F:65])[CH:59]=2)[N:49]=1.[N:68]1([CH:83]2[CH2:88][CH2:87][NH:86][CH2:85][CH2:84]2)[CH2:73][CH2:72][CH:71]([O:74]C(=O)C2C=CC=CC=2)[CH2:70][CH2:69]1>>[CH3:57][C:52]1[C:53]([C:54]([N:86]2[CH2:85][CH2:84][CH:83]([N:68]3[CH2:73][CH2:72][CH:71]([OH:74])[CH2:70][CH2:69]3)[CH2:88][CH2:87]2)=[O:56])=[C:48]([CH3:47])[N:49]=[C:50]([C:58]2[CH:63]=[CH:62][CH:61]=[C:60]([C:64]([F:65])([F:66])[F:67])[CH:59]=2)[N:51]=1

参加物

5

反応物 4

HCID 44473778(4-Bromo-2,6-dimethyl-phenyl)-[4-((S)-2-hydroxymethyl-pyrrolidin-1-yl)-piperidin-1-yl]-methanoneHCID 627447164,6-Dimethyl-2-(3-trifluoromethyl-phenyl)-pyrimidine-5-carboxylic acid2 回HCID 66901535Benzoic acid [1,4']bipiperidinyl-4-yl esterHCID 66901599(4-Bromo-2,6-dimethyl-phenyl)-(4-pyrrolidin-1-yl-piperidin-1-yl)-methanone

生成物 1

HCID 57580525[4,6-Dimethyl-2-(3-trifluoromethyl-phenyl)-pyrimidin-5-yl]-(4-hydroxy-[1,4']bipiperidinyl-1'-yl)-methanone

実験手順

In analogy to the procedures described for intermediate 1 and for intermediate 4 B, 4,6-dimethyl-2-(3-trifluoromethyl-phenyl)-pyrimidine-5-carboxylic acid (intermediate 5) was converted into its acid chloride, reacted with benzoic acid [1,4′]bipiperidinyl-4-yl ester (example 22) and subsequently saponified to give the title compound as colorless solid. MS: 463.3 (MH+).

出典と根拠

ORDレコード
ord-5d265573b39e475b87d4da89aebff45c
出典データセット
uspto-grants-2012_04
特許番号
US08153805B2

関連ノート

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