Array Biopharma Inc.

Astrazeneca Ab

Astrazeneca Sb

Simon Mark Pointon

James Gair Ford

Anthony D Piscopio

John A DeMattei

Sagar Raj Shakya

Bruno P Hache

John Leonard

Matthew Charles Evans

Koen Peeters

Timothy John Lilley

James Francis McCabe

Lyn Powell

Mark Purdie

Philip O'Keefe

Jane Withnall

Anne O'Kearney-McMullan

James Francis Mccabe

John Demattei

Anne O'kearney-Mcmullan

Philip O'keefe

Sagar Shakya

Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X, R, Rand Rare as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.

Processes for preparing benzimidazole compounds

Provided are compounds having Formula VIIIa-1: wherein Z, X, R, Rand Rare as defined herein. Compounds of Formula VIIIa-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Benzimidazole compounds

Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1: wherein Z, X, X, X, Rand Rare as defined herein. Compounds of Formula Ib-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Process for preparing benzimidazole compounds

The present invention relates to chemical processes useful in the manufacture of the compound 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline (the active entity within AZD0530), to intermediates useful in the manufacture of that compound and to processes for the manufacture of those intermediates. The invention also relates to particular crystalline forms of that compound such as a difumarate salt and a trihydrate and to pharmaceutical compositions containing such crystalline forms.

Crystalline forms of 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline

Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X, X, X, Rand Rare as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives. 

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Macclesfield, United Kingdom

Simon Mark Pointon