反应详情

0.42 cm3 of triethylamine and 0.49 g of carbonyldiimidazole are added to a solution, cooled to +4° C., of 0.86 g of (2-pyrrolidinophenyl)acetic acid hydrobromide in 20 cm3 of dry dichloromethane. The mixture is stirred for one hour at +4° C. and then a solution of 1 g of (3aR,4S,7aR)-7,7-diphenyl-4-perhydroisoindolol hydrochloride and 0.42 cm3 of triethylamine in 10 cm3 of dry dichloromethane is added. The reaction mixture is stirred at room temperature for 24 hours and then then washed twice with 10 cm3 of water and then with an aqueous solution of sodium hydrogen carbonate, dried over magnesium sulphate, filtered and concentrated to dryness under reduced pressure (2.7 kPa). The product, which is obtained in the form of a base, is converted to the hydrochloride by dissolving in a minimum amount of acetone and treating with a solution of hydrochloric acid in ethyl ether and adding ethyl ether. The solid obtained is triturated in ethyl ether and then dried. 0.2 g of (3aR,4S,7aR)-7,7-diphenyl-2-[(2-pyrrolidinophenyl)acetyl]-4-perhydroisoindolol hydrochloride is obtained in the form of a beige solid.

1. stirringThe reaction mixture is stirred at room temperature for 24 hours
2. washwashed twice with 10 cm3 of water
3. dry with materialwith an aqueous solution of sodium hydrogen carbonate, dried over magnesium sulphate
4. filtrationfiltered
5. concentrationconcentrated to dryness under reduced pressure (2.7 kPa)
6. customThe product, which is obtained in the form of a base
7. customThe solid obtained
8. customis triturated in ethyl ether
9. customdried