Preparation of dihydrothieno [3, 2-d] pyrimidines and...

C - Chemistry – Metallurgy – 07 – D

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C07D 495/04 (2006.01)

Patent

CA 2702500

The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof,(I) wherein X is SO or SO2, preferably SO, and wherein R A, R1, R2, R3, R4 and R5 have the meanings given in the description. The methods according to this invention are more suitable for large-scale synthesis of said compounds than prior methods because the new synthetic process avoids distillation and chromatographic purification between steps and results in a higher overall yield of the desired product.

La présente invention concerne des procédés améliorés de préparation de dihydrothiénopyrimidines de formule 1, et des intermédiaires de celles-ci,(I) X représentant SO ou SO2, de préférence SO, et RA, R1, R2, R3, R4 et R5 ayant les significations données dans la description. Les procédés selon cette invention sont plus appropriés pour une synthèse à large échelle desdits composés que les procédés antérieurs car le nouveau procédé de synthèse évite la distillation et la purification chromatographique entre les étapes et résulte en un rendement total plus élevé du produit désiré.

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