Water → 2-[2-(4-fluoro-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-(hexahydrocyclopenta[1,4]oxazin-4-yl)-3H-pyrimidin-4-one

HRID 2278534ノート

反応式

HRID 2278534 の反応式
Cl.[O:2]1[C:7]2=[CH:8][CH2:9][CH2:10][CH:6]2[NH:5][CH2:4][CH2:3]1.[F:11][C:12]1[CH:20]=[CH:19][CH:18]=[C:17]2[C:13]=1[CH2:14][CH2:15][N:16]2[C:21](=[O:31])[CH2:22][C:23]1[NH:28][C:27](=[O:29])[CH:26]=[C:25](Cl)[N:24]=1.O>C(N(C(C)C)CC)(C)C>[F:11][C:12]1[CH:20]=[CH:19][CH:18]=[C:17]2[C:13]=1[CH2:14][CH2:15][N:16]2[C:21](=[O:31])[CH2:22][C:23]1[NH:28][C:27](=[O:29])[CH:26]=[C:25]([N:5]2[CH:6]3[CH2:10][CH2:9][CH2:8][CH:7]3[O:2][CH2:3][CH2:4]2)[N:24]=1

参加物

5

反応物 3

HCID 962WaterHCID 86699266Hexahydrocyclopenta[1,4]oxazine hydrochlorideHCID 1363786742-[2-(4-fluoro-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-chloro-3H-pyrimidin-4-one

生成物 1

HCID 1360984712-[2-(4-fluoro-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-(hexahydrocyclopenta[1,4]oxazin-4-yl)-3H-pyrimidin-4-one収率 23.2%

試薬・触媒・溶媒 1

HCID 81531Diisopropylethylamine溶媒

反応条件

温度
100 °C

実験手順

532 mg of hexahydrocyclopenta[1,4]oxazine hydrochloride are added to a solution of 100 mg of 2-[2-(4-fluoro-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-chloro-3H-pyrimidin-4-one in 5 ml of diisopropylethylamine. The reaction medium is heated at 100° C. for 2 hours. The reaction medium is taken up with 10 ml of water. The solid formed is filtered off and washed with water and then dried so as to give 30 mg of 2-[2-(4-fluoro-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-(hexahydrocyclopenta[1,4]oxazin-4-yl)-3H-pyrimidin-4-one in the form of a beige solid, the characteristics of which are the following:

後処理

  1. customThe solid formed
  2. filtrationis filtered off
  3. washwashed with water
  4. customdried so as

出典と根拠

ORDレコード
ord-48dec5e59ef6451ea1c318e24143a050
出典データセット
uspto-grants-2015_09
特許番号
US09133168B2

反応ノート

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