Worldwide Process Research and Development

Phoenixville, PA, United States

Worldwide Process Research and Development

Phoenixville, PA, United States

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Wang Y.,Worldwide Process Research and Development | Przyuski K.,Worldwide Process Research and Development | Roemmele R.C.,Worldwide Process Research and Development | Hudkins R.L.,Discovery Research | Bakale R.P.,Worldwide Process Research and Development
Organic Process Research and Development | Year: 2013

The evolution of the process to prepare CEP-32215, 3-(1′- cyclobutylspiro[4H-1,3-benzodioxine-2,4′-piperidine]-6-yl)-5,5-dimethyl-1, 4-dihydropyridazine-6-one, is presented. Two routes detailing preparation of supplies for biological screening are discussed along with the optimized fit-for-purpose process used to prepare several hundred grams for preclinical testing. Details on the development of the formation of the key spiroketal moiety are presented along with the discovery of a novel Suzuki coupling approach for synthesis of the backbone of the molecule. © 2013 American Chemical Society.

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