反応 #69628

反応方程式

hydrochloride monohydrate

compound IV

hydrochloride monohydrate

ethyl-N-(6-amino-2,3-dichlorobenzyl)glycine

compound I

ethyl-N-(6-amino-2,3-dichlorobenzyl)glycine

cyanogen bromide

anagrelide

cyanogen bromide

→

compound II

iminoquinazoline

溶媒

toluene

反応条件

実験手順

Commercially, as discussed in U.S. Pat. No. 5,801,245, and as shown in FIG. 1, anagrelide has been prepared as the hydrochloride monohydrate (compound IV) from the intermediate, ethyl-N-(6-amino-2,3-dichlorobenzyl)glycine (compound I) either by reaction with cyanogen bromide in hot alcoholic solution, or, preferentially, by reaction with cyanogen bromide in an aprotic solvent such as toluene to give the iminoquinazoline intermediate (compound II), which is isolated and then reacted with a base in a hot solution of alcohol to form anagrelide base (compound III).

出典