Morpholine → 4-amino-2-morpholin-4-yl-pyrimidine-5-carboxylic Acid

反応式

[NH2:1][C:2]1[C:7]([C:8]([OH:10])=[O:9])=[CH:6][N:5]=[C:4](SCC)[N:3]=1.[NH:14]1[CH2:19][CH2:18][O:17][CH2:16][CH2:15]1>>[NH2:1][C:2]1[C:7]([C:8]([OH:10])=[O:9])=[CH:6][N:5]=[C:4]([N:14]2[CH2:19][CH2:18][O:17][CH2:16][CH2:15]2)[N:3]=1

参加物

反応物 2

HCID 8083Morpholine

HCID 2753004-Amino-2-(ethylthio)pyrimidine-5-carboxylic acid

生成物 1

HCID 99209194-amino-2-morpholin-4-yl-pyrimidine-5-carboxylic Acid収率 30%

反応条件

温度: 80 °C

実験手順

A mixture of 4-amino-5-carboxy-2-ethylmercaptopyrimidine (0.35 g, 1.8 mmol) and morpholine (0.5 mL, 10 mmol) was warmed at 80° C. for 4 d and concentrated in vacuo. The residue was purified by flash chromatography (silica gel, 4×7.5 cm, eluted with 97.25/2.5/0.25 acetonitrile/water/acetic acid) to yield the product as a white solid (34 mg, 30%).

後処理

concentrationconcentrated in vacuo
customThe residue was purified by flash chromatography (silica gel, 4×7.5 cm, eluted with 97.25/2.5/0.25 acetonitrile/water/acetic acid)

出典と根拠

ORDレコード: ord-3a48034418864f6d8827d4424033bd31
出典データセット: uspto-grants-2012_08
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08242115B2

反応ノート

読み込み中…