3-Morpholinecarboxylic acid → 4-((6-(2-Chloro-4-fluorophenyl)-5-(ethoxycarbonyl)-3-methyl-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholine-3-carboxylic acid

HRID 524622

反応式

HRID 524622 の反応式
Br[CH2:2][C:3]1[N:8]([CH3:9])[C:7]([C:10]2[S:11][CH:12]=[CH:13][N:14]=2)=[N:6][CH:5]([C:15]2[CH:20]=[CH:19][C:18]([F:21])=[CH:17][C:16]=2[Cl:22])[C:4]=1[C:23]([O:25][CH2:26][CH3:27])=[O:24].[NH:28]1[CH2:33][CH2:32][O:31][CH2:30][CH:29]1[C:34]([OH:36])=[O:35]>>[Cl:22][C:16]1[CH:17]=[C:18]([F:21])[CH:19]=[CH:20][C:15]=1[CH:5]1[N:6]=[C:7]([C:10]2[S:11][CH:12]=[CH:13][N:14]=2)[N:8]([CH3:9])[C:3]([CH2:2][N:28]2[CH2:33][CH2:32][O:31][CH2:30][CH:29]2[C:34]([OH:36])=[O:35])=[C:4]1[C:23]([O:25][CH2:26][CH3:27])=[O:24]

参加物

3

反応物 2

HCID 33401523-Morpholinecarboxylic acidHCID 118107629Ethyl 6-(bromomethyl)-4-(2-chloro-4-fluorophenyl)-1-methyl-2-(thiazol-2-yl)-1,4-dihydropyrimidine-5-carboxylate

生成物 1

HCID 900439014-((6-(2-Chloro-4-fluorophenyl)-5-(ethoxycarbonyl)-3-methyl-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholine-3-carboxylic acid収率 20%

実験手順

Ethyl 6-(bromomethyl)-4-(2-chloro-4-fluorophenyl)-1-methyl-2-(thiazol-2-yl)-1,4-dihydropyrimidine-5-carboxylate (0.48 g, 1.02 mmol) was reacted with morpholine-3-carboxylic acid (0.4 g, 3.06 mmol) according to the procedure as described in Example 1, Step C to give the title compound as a yellow solid (0.1 g, 20%). The compound was characterized by the following spectroscopic data:

出典と根拠

ORDレコード
ord-a7d7a7377c5b421e9ba1bfd370728e62
出典データセット
uspto-grants-2016_05
特許番号
US09340538B2

関連ノート

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