Array Biopharma Inc.

Astrazeneca Ab

Astrazeneca Sb

Koen Peeters

Anthony D Piscopio

John A DeMattei

Sagar Raj Shakya

James Gair Ford

Bruno P Hache

John Leonard

Matthew Charles Evans

Simon Mark Pointon

Timothy John Lilley

Jean-Paul Dejonghe

Marc Renard

John Demattei

Timothy John Astrazeneca Ab Lilley

James Gair Astrazeneca Ab Ford

John Astrazeneca Ab Leonard

Matthew Charles Pdlsw2 PR&D Office Um2 Astrazeneca Evans

Simon Mark Astrazeneca Ab Pointon

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

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. 

The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure trans-cyclopropane carboxylic acid derivatives, processes for preparing the carboxylic acid derivatives and their use in preparing pharmaceuticals.

Chemical process for preparation of intermediates

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Wetteren, Belgium

Koen Peeters