Millennium Pharmaceuticals Limited

Hiro Mizutani

Steven P Langston

Lei Zhu

Quentin J McCubbin

Eric L Elliott

Marianne Langston

Matthew Stirling

Ian G Armitage

The present invention provides processes and synthetic intermediate (Ia) for the synthesis of 4-substituted ((1S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates. These sulfamate compounds are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity. 

Process for the synthesis of E1 activating enzyme inhibitors

The present invention provides sulfamoylating reagents of formula RN&#x2014;S(O)X, wherein X is a cyclic tertiary amine or a nitrogen-containing heteroaryl and Ris an amine protecting group or hydrogen.

Sulfamoylating reagents

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Cambridge, MA, United States of America

Hiro Mizutani