反应详情

A solution of 150 mg (0.40 mmol) of 6-amino-N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-1-benzothiophene-2-carboxamide dihydrochloride and 48 μl (0.65 mmol) of acetone in 1.5 ml of 1,2-dichloroethane is adjusted to pH 4 using acetic acid. 254.8 mg (1.20 mmol) of sodium triacetoxyborohydride are added, and the mixture is stirred at RT for 6 h. The contents of the flask are concentrated under reduced pressure and purified by preparative HPLC. The product fractions are concentrated and the residue is dissolved in a 5:1 mixture of acetonitrile and 1N hydrochloric acid, then again concentrated and dried under high vacuum. 49 mg (29.4% of theory) of the title compound are obtained.

1. concentrationThe contents of the flask are concentrated under reduced pressure
2. custompurified by preparative HPLC
3. concentrationThe product fractions are concentrated
4. dissolutionthe residue is dissolved in a 5:1 mixture of acetonitrile and 1N hydrochloric acid
5. concentrationagain concentrated
6. customdried under high vacuum