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3-chloro-6-Methoxy-[1,5]-naphthyridin-4-ol synthesis

3synthesis methods
-

Yield:724787-12-6 80%

Reaction Conditions:

with N-chloro-succinimide in acetic acid at 35; for 24 h;

Steps:

1.a

A solution of 6-(methyloxy)-l,5-naphthyridin-4-ol (6-methoxy-lH- [l,5]naphthyridin-4-one, for a synthesis see WO2002096907 Example 1) (50 g; 0.2841 mol) in glacial acetic acid (750 niL) was treated with N-chlorosuccinimide (42.5 g; 0.3185 mol) and the mixture was heated under argon at 350C for 24 hours. It was cooled and the precipitated solid filtered off and washed with a little cold acetic acid, then ether and finally hexane. It was dried at 5O0C overnight in vacuo to give an off-white solid 48g (80%). LC/MS (+ve ion electrospray): m/z 209/211 (M+η)+

References:

WO2008/6648,2008,A1 Location in patent:Page/Page column 23