Morpholine → 8-[2-(4-Isopropyl-1,3-thiazol-2-yl)ethyl)-2-morpholino-3-(1-p-methoxybenzyl-1,2,3,4-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one

HRID 1828512ノート

反応式

HRID 1828512 の反応式
[CH:1]([C:4]1[N:5]=[C:6]([CH2:9][CH2:10][C:11]2[CH:46]=[CH:45][N:14]3[C:15](=[O:44])[C:16]([C:30]4[N:34]([CH2:35][C:36]5[CH:41]=[CH:40][C:39]([O:42][CH3:43])=[CH:38][CH:37]=5)[N:33]=[N:32][N:31]=4)=[C:17](OS(C4C=CC(C)=CC=4)(=O)=O)[N:18]=[C:13]3[CH:12]=2)[S:7][CH:8]=1)([CH3:3])[CH3:2].[NH:47]1[CH2:52][CH2:51][O:50][CH2:49][CH2:48]1>O1CCCC1>[CH:1]([C:4]1[N:5]=[C:6]([CH2:9][CH2:10][C:11]2[CH:46]=[CH:45][N:14]3[C:15](=[O:44])[C:16]([C:30]4[N:34]([CH2:35][C:36]5[CH:41]=[CH:40][C:39]([O:42][CH3:43])=[CH:38][CH:37]=5)[N:33]=[N:32][N:31]=4)=[C:17]([N:47]4[CH2:52][CH2:51][O:50][CH2:49][CH2:48]4)[N:18]=[C:13]3[CH:12]=2)[S:7][CH:8]=1)([CH3:3])[CH3:2]

参加物

4

反応物 2

HCID 8083MorpholineHCID 220635268-[2-(4-Isopropyl-1,3-thiazol-2-yl)ethyl]-2-tosyloxy-3-[(4-methoxybenzyl)tetrazol-5-yl]-4H-pyrido[1,2-a]pyrimidin-4-one2 回

生成物 1

HCID 696031968-[2-(4-Isopropyl-1,3-thiazol-2-yl)ethyl)-2-morpholino-3-(1-p-methoxybenzyl-1,2,3,4-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one収率 59%

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒

実験手順

The 8-[2-(4-isopropyl-1,3-thiazol-2-yl)ethyl]-2-tosyloxy-3-[(4-methoxybenzyl)-tetrazol-5-yl]-4H-pyrido[1,2-a]pyrimidin-4-one (61 mg) obtained in (B) was dissolved in tetrahydrofuran (1 ml), added with morpholine (40 ml) at room temperature, and stirred overnight at the same temperature. After the solvent was evaporated under reduced pressure, the residue was purified by silica gel column chromatography to obtain the title compound (31 mg, 59%).

後処理

  1. customAfter the solvent was evaporated under reduced pressure
  2. customthe residue was purified by silica gel column chromatography

出典と根拠

ORDレコード
ord-48c33a157dd745b2a23c20d3d916376d
出典データセット
uspto-grants-2006_06
特許番号
US07056917B2

反応ノート

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