Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Sodium Carbonate | HCID 10340 | — |
| Edukt | 6-(2-chloroethyl)-7-methyl-5H-(1,3)thiazolo(3,2-a)pyrimidin-5-one | HCID 817872 | — |
| Edukt | 1-(Piperidin-4-yl)-1H-indole | HCID 14090755 | — |
| Katalysator | Potassium Iodide | HCID 4875 | — |
| Lösungsmittel | Methyl Isobutyl Ketone | HCID 7909 | — |
| Produkt | HCID 70004001 | HCID 70004001 | 51,4% |
Reaktionsschritte
A mixture of 1-(4-piperidinyl)-1H-indole (4.1 g), 6-(2-chloroethyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one (3.4 g), prepared as described in EP-A-0,196,132, sodium carbonate (6 g) and potassium iodide (0.1 g) in 4-methyl-2-pentanone (250 ml) was stirred and refluxed overnight. The warm reaction mixture was filtered and the filtrate was evaporated. The residue was purified over silica gel on a glass filter (eluent: CH2Cl2 /C2H5OH 90/10). The pure fractions were collected and the solvent was evaporated. The residue was crystallized from DIPE with a small amount of CH3CN. The precipitate was filtered off and dried, yielding 3 g (51%) 6-[2-[4-(1H-indol-1-yl)-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one (compound 3; mp. 134.4° C.).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patentnummer | US05919788 |
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| Quelldatensatz | uspto-grants-1999_07 |
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| ORD ID | ord-eb63fc27d2a94fc989572b3e79e0be3c |
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| Quellennotiz | uspto-grants-1999_07 |
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