Reaktion #1728536

Reaktionsgleichung

water

4-chloro-2-[4-(4-chloro-phenyl)-piperazin-1-yl]-6,7-dihydro-thieno[3,2-d]pyrimidine 5-oxide

(R)-1-(6-chloro-1H-benzimidazol-2-yl)-2-methoxy-ethylamine

diisopropylethylamine

→

product

(1R,2R)-1-(6-chloro-1H-benzimidazol-2-yl)-1-{2-[4-(4-chloro-phenyl)-piperazin-1-yl]-5-oxo-6,7-dihydro-5H-5λ4-thieno[3,2-d]pyrimidin-4-ylamino}-propan-2-ol

Lösungsmittel

dichloromethane

dioxane

Reaktionsbedingungen

Aufarbeitung

1. 1
   Extraktionextracted
2. 2
   SonstigeThe product is purified by semipreparative HPLC (method A)

Vorschrift

200 mg 4-chloro-2-[4-(4-chloro-phenyl)-piperazin-1-yl]-6,7-dihydro-thieno[3,2-d]pyrimidine 5-oxide (cf Example 124), 353.41 mg (R)-1-(6-chloro-1H-benzimidazol-2-yl)-2-methoxy-ethylamine and 179.62 μl diisopropylethylamine are placed in 4 ml dioxane, heated to 120° C. in the microwave for 2×0.3 hours. Then the reaction mixture is combined with water and dichloromethane and extracted. The product is purified by semipreparative HPLC (method A). 150 mg of the product are obtained as a powder. Analytical HPLC-MS (method B): RT=1.90 min.

Quelle