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CAPLUS COPYRIGHT 2011 ACS
||A process for preparing intermediate compounds useful for producing dolasetron
||Perez Andres, Juan Antonio; Dalmases Barjoan, Pere; Huguet Clotet, Joan
||Inke, S.A., Spain
||U.S. Pat. Appl. Publ., 20pp. CODEN: USXXCO
The invention relates to a process for the preparation of compds. I (wherein R1 is alkyl, R2 and R3 are independently alkyl, or both R2 and R3 attached resp. to the oxygen atoms belonging to the same carbon atom form a cycle), which are useful for producing dolasetron. For instance, the compound I (R1 = R2 = R3 = Me) was prepared by substitution of di-Me malonate with bromoacetaldehyde di-Me acetal followed by dealkoxycarbonylation in 75% yield, which was converted to dolasetron in about 5 steps.