Method for the manufacture of anagrelide

Details Method for the manufacture of anagrelide Method for the manufacture of anagrelide

C - Chemistry, Metallurgy

07

D

C07D 487/00 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2417001

Methods are provided for making certain 6,7-dihaol-1,5-dihydroimidazo [2,1- b]quinazolin-2(3H)-ones from 2,3-dihalobenzaldehydes. A method is also provided for making the intermediate ethyl N-(2,3-dihalo-6- nitrobenzyl)glycines from 2,3-dihalobenzaldehydes and for reducing the glycine compounds using either SnC12 or a specially defined catalyst. A cyclization method to form the desired 6,7-dihalo-1,5-dihydroimidazo[2,1-b]quinazolin- 2(3H)-ones from the corresponding iminquinazoline compounds is further provided. These methods are particularly suitable in the manufacture of Anagrelide base.

L'invention concerne des procédés destinés à préparer certaines 6,7-dihalo-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-ones à partir de 2,3-dihalobenzaldéhydes. L'invention se rapporte également à un procédé destiné à préparer les produits intermédiaires éthyl-N-(2,3-dihalo-6-nitrobenzyl)glycines à partir de 2,3-dihalobenzaldéhydes et à réduire les composés glycine avec du SnCl¿2? ou un catalyseur spécialement défini. L'invention concerne en outre un procédé de cyclisation destiné à former les 6,7-dihalo-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-ones souhaitées à partir des composés iminoquinazoline correspondants. Ces procédés conviennent notamment à la préparation d'une base anagrélide.

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