Synthesis of dihydrothieno[3,2-d]pyrimidine diols

US8471010B2 · kind B2 · utility

Assignee

• Boehringer Ingelheim International GmbH · DE

Inventors

• Rogelio P. Frutos · Sandy Hook, US
• Thomas G. Tampone · Southbury, US
• Jason Alan Mulder · New Milford, US
• Dhileepkumar Krishnamurthy · Westborough, US
• Chris Hugh Senanayake · Brookfield, US

Key dates

• Filing date: May 7, 2009
• Grant date: Jun 25, 2013
• Expiry date: Jan 12, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D239/70
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to an improved process for the preparation of dihydrothieno[3,2-d]pyrimidine diols, and similar pyrimidine diols, that is efficient, high-yielding, and does not require expensive and potentially unstable intermediates. The diols are used as intermediates in the synthesis of pyrimidine compounds which inhibit PDE4, and are thus useful in the treatment of respiratory or gastrointestinal diseases and complaints, peripheral or central nervous system diseases and disorders, inflammatory conditions, and cancers.