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

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 239/70 (2006.01) C07D 495/04 (2006.01)

Patent

CA 2722970

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.

La présente invention concerne un procédé amélioré de préparation de diols dihydrothiénol[3,2-d]pyrimidiniques et de diols pyrimidiniques analogues. Ce procédé est efficace, présente un rendement élevé et ne requiert pas de produits intermédiaires coûteux et potentiellement instables. Les diols sont utilisés comme produits intermédiaires dans la synthèse de composés pyrimidiniques inhibant la PDE4, et sont donc utiles dans le traitement de maladies et de plaintes respiratoires ou gastro-intestinales, de maladies et de troubles du système nerveux central ou périphérique, d'affections inflammatoires et de cancers.

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