Reaktion #1065632

Reaktionsgleichung

[1-(2-aminoethyl)-4-piperidinyl](4-fluorophenyl)methanone

ethyl 2-isothiocyanato-4-(phenylmethoxy)benzoate

→

3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2,3-dihydro-7-(phenylmethoxy)-2-thioxo-4(1H)-quinazolinone

Ausbeute 29.0%

Lösungsmittel

tetrahydrofuran

tetrahydrofuran

Reaktionsbedingungen

Aufarbeitung

1. 1
   Temperaturat reflux temperature
2. 2
   TemperaturAfter cooling
3. 3
   Filtrationthe product was filtered off
4. 4
   Sonstigecrystallized from a mixture of N,N-dimethylformamide and water
5. 5
   FiltrationThe product was filtered off
6. 6
   Sonstigedried

Vorschrift

To a stirred mixture of 6.25 parts of [1-(2-aminoethyl)-4-piperidinyl](4-fluorophenyl)methanone and 135 parts of tetrahydrofuran was added dropwise a solution of 7.5 parts of ethyl 2-isothiocyanato-4-(phenylmethoxy)benzoate in 45 parts of tetrahydrofuran. Upon completion, stirring was continued for 4 hours at room temperature and for 30 minutes at reflux temperature. After cooling, the product was filtered off and crystallized from a mixture of N,N-dimethylformamide and water. The product was filtered off and dried, yielding 3.8 parts (29%) of 3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2,3-dihydro-7-(phenylmethoxy)-2-thioxo-4(1H)-quinazolinone; 236.0° C. (dec.) (6).

Quelle