4-Aminotetrahydropyran → 2-[(E)-2-(3-Butyl-5-methyl-isoxazol-4-yl)-vinyl]-4-methyl-thiazole-5-carboxylic acid (tetrahydro-pyran-4-yl)-amide

HRID 1923611ノート

反応式

HRID 1923611 の反応式
CO[C:3]([C:5]1[S:9][C:8](/[CH:10]=[CH:11]/[C:12]2[C:13]([CH2:18][CH2:19][CH2:20][CH3:21])=[N:14][O:15][C:16]=2[CH3:17])=[N:7][C:6]=1[CH3:22])=[O:4].[NH2:23][CH:24]1[CH2:29][CH2:28][O:27][CH2:26][CH2:25]1>>[O:27]1[CH2:28][CH2:29][CH:24]([NH:23][C:3]([C:5]2[S:9][C:8](/[CH:10]=[CH:11]/[C:12]3[C:13]([CH2:18][CH2:19][CH2:20][CH3:21])=[N:14][O:15][C:16]=3[CH3:17])=[N:7][C:6]=2[CH3:22])=[O:4])[CH2:25][CH2:26]1

参加物

3

反応物 2

HCID 4192234-AminotetrahydropyranHCID 666436512-[(E)-2-(3-Butyl-5-methyl-isoxazol-4-yl)-vinyl]-4-methyl-thiazole-5-carboxylic acid methyl ester

生成物 1

HCID 497811522-[(E)-2-(3-Butyl-5-methyl-isoxazol-4-yl)-vinyl]-4-methyl-thiazole-5-carboxylic acid (tetrahydro-pyran-4-yl)-amide収率 75%

実験手順

As described for example 93d, 2-[(E)-2-(3-butyl-5-methyl-isoxazol-4-yl)-vinyl]-4-methyl-thiazole-5-carboxylic acid methyl ester (60 mg, 0.19 mmol) was converted, using 4-aminotetrahydropyran instead of isopropylamine, to the title compound (55 mg, 75%) which was obtained as a white solid. MS: m/e=390.3 [M+H]+.

出典と根拠

ORDレコード
ord-189d06f116dd42a79fe860d250fde6de
出典データセット
uspto-grants-2012_05
特許番号
US08178522B2

反応ノート

読み込み中…