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 1828512Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1828512
[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]

Komponenten

4

Edukt 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×

Produkt 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-oneAusbeute 59 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 8028TetrahydrofuranLösungsmittel

Versuchsvorschrift

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%).

Aufarbeitung

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

Quellen und Nachweise

ORD-Eintrag
ord-48c33a157dd745b2a23c20d3d916376d
Quelldatensatz
uspto-grants-2006_06
Patentnummer
US07056917B2

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