Diisopropylethylamine → Ethyl 2-(4-aminopiperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylate

HRID 43931

反応式

HRID 43931 の反応式
[NH2:1][CH:2]1[CH2:7][CH2:6][NH:5][CH2:4][CH2:3]1.Br[C:9]1[S:10][C:11]([C:15]([O:17][CH2:18][CH3:19])=[O:16])=[C:12]([CH3:14])[N:13]=1.C(N(C(C)C)CC)(C)C>>[NH2:1][CH:2]1[CH2:7][CH2:6][N:5]([C:9]2[S:10][C:11]([C:15]([O:17][CH2:18][CH3:19])=[O:16])=[C:12]([CH3:14])[N:13]=2)[CH2:4][CH2:3]1

参加物

4

反応物 3

HCID 81531DiisopropylethylamineHCID 4243614-PiperidinamineHCID 2824057Ethyl 2-bromo-4-methyl-1,3-thiazole-5-carboxylate

生成物 1

HCID 67548556Ethyl 2-(4-aminopiperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylate収率 87.6%

実験手順

The same operation as in Example (237a) was performed using 4-aminopiperidine (0.19 mL, 1.80 mmol), ethyl 2-bromo-4-methylthiazole-5-carboxylate (300 mg, 1.20 mmol) and diisopropylethylamine (0.42 mL, 2.40 mmol), to obtain 283 mg of the title compound as a pale yellow oily substance (88%).

出典と根拠

ORDレコード
ord-73afe5373f8742218418f04cf9ebd489
出典データセット
uspto-grants-2013_09
特許番号
US08536197B2

関連ノート

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