Processes for the preparation of furazanobenzimidazoles and crystalline forms thereof
AssigneeBasilea Pharmaceutica International AG
InventorsGregor Welti, Markus Heubes, David Tagliaferri
Life of this patent
Estimating the term…
Abstract
The present invention provides processes for preparing a compound of formula (I) and pharmaceutically acceptable salts thereof, comprising deprotecting a compound of formula (II), wherein each R3 independently represents a tertiary alkyl group, preferably wherein each R3 is tertiary butyl. The invention also provides intermediates useful for preparing compounds of formula (I) and processes for preparing these intermediates. Additionally the invention provides polymorphic forms of the dichloride salt of the compound of formula (I) and their use in the treatment of proliferative disorders.
Claims32
A process for preparing a compound of formula I:
- or a pharmaceutically acceptable salt thereof, comprising the step of deprotecting a compound of formula II:
- wherein each R3 independently is a tertiary alkyl group and
- wherein the step of deprotecting the compound of formula II is performed under acidic conditions and is performed in a solvent selected from acetone and tetrahydrofuran.
A process for preparing a compound of formula II
- wherein each R3 independently is a tertiary alkyl group;
- comprising reacting a compound of formula III
- wherein R1 is chloro
- wherein each R3 independently is a tertiary alkyl group;
- with a compound of formula IV
A process for preparing a compound of formula III
- wherein each R3 independently is a tertiary alkyl group and wherein R1 is chloro, comprising the step of reacting a compound of formula V
- wherein R2 is OH;
- and
- wherein each R3 independently is a tertiary alkyl group;
- with a compound of formula VI
- wherein R1a is chloro.
Dependencies are inferred from the claim text.