BIIB055 was being developed as a first in class treatment for RA at Biogen Idec. Phase 1 supplies were prepared by two routes establishing the three stereogenic centers in the molecule. The presentation will discuss both routes in detail for producing multi-kilogram quantities of BIIB055.The key points to be addressed are the preparation of two key intermediates for establishing the stereogenic centers. The reductive amination-cyclization sequence for establishing the lactam ring and the critical reaction conditions required for maintaining the lactam stereogenic center

Rapid development and scale up of two routes for the preparation of BIIB055

248th National Meeting (2014)

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