反応式
[F:1][C:2]([F:12])([F:11])[C:3]1[CH:10]=[CH:9][CH:8]=[CH:7][C:4]=1[CH2:5][OH:6].[C:13](C1NC=CN=1)(C1NC=CN=1)=[O:14].[Br:25][C:26]1[CH:27]=[CH:28][CH:29]=[C:30]2[C:39]=1[C:33]1([CH2:38][CH2:37][NH:36][CH2:35][CH2:34]1)[CH2:32][C:31]2=[O:40]>C(Cl)Cl>[Br:25][C:26]1[CH:27]=[CH:28][CH:29]=[C:30]2[C:39]=1[C:33]1([CH2:34][CH2:35][N:36]([C:13]([O:6][CH2:5][C:4]3[CH:7]=[CH:8][CH:9]=[CH:10][C:3]=3[C:2]([F:11])([F:12])[F:1])=[O:14])[CH2:37][CH2:38]1)[CH2:32][C:31]2=[O:40]参加物
5
反応物 3
生成物 1
試薬・触媒・溶媒 1
実験手順
To o-(trifluoromethyl)benzyl alcohol (35 mg, 0.20 mmol) in CH2Cl2 (4 mL) was added was a solution of carbonyl diimidazole (29 mg, 0.18 mmol) in CH2Cl2 (4 mL). The mixture was stirred at rt for 2 h. A 1-mL aliquot of the resulting solution (0.05 mmol) was added to a solution 7-bromospiro[indene-1,4′-piperidin]-3(2H)-one (14.5 mg, 0.05 mmol) in CH2Cl2 (1 mL). The mixture was stirred at rt for 16 h, concentrated, redissolved in MeCN (1 mL) and heated at 60° C. for 2 h. Prep HPLC afforded the title compound. LC-MS Method 1 tR=2.06, min, m/z=484, 482.
後処理
- stirringThe mixture was stirred at rt for 16 h
- concentrationconcentrated
- dissolutionredissolved in MeCN (1 mL)
- temperatureheated at 60° C. for 2 h
出典と根拠
- ORDレコード
- ord-67ab8ad46ead4b3d99d43255073f14ae
- 出典データセット
- uspto-grants-2013_02
- 特許番号
- US08383629B2
関連ノート
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