反应详情

The process is performed under the conditions of Example 1 starting with 0.46 g of N-(tert-butyl)-N′-[(1R)-2-hydroxy-1-(4-pyridylmethyl)ethyl]thiourea which is heated in 5 cm3 of aqueous 5 N hydrochloric acid for 16 hours at a temperature in the region of 100° C. After concentration of the reaction mass under reduced pressure (5 kPa) at a temperature in the region of 40° C., an oil is obtained which is taken up in 3 cm3 of 2-propanol. The resulting crystalline precipitate is spin-filtered, washed with 2-propanol and air-dried. 0.1 g of (+)-(4R)-4-(4-pyridylmethyl)-4,5-dihydro-1,3-thiazol-2-ylamine dihydrochloride is obtained in the form of an orange-colored solid melting at 150° C. (αD20=+38.3±0.9 at a concentration of 0.5% in MeOH).

1. customAfter concentration of the reaction mass under reduced pressure (5 kPa) at a temperature in the region of 40° C., an oil is obtained which
2. filtrationThe resulting crystalline precipitate is spin-filtered
3. washwashed with 2-propanol
4. customair-dried