| abstract |
The present invention provides a new, easily implemented in industry and cost-effective method, containing only a small number of stages and based on the use of new intermediate products, to obtain 1- (4-3 (R) - [3 (S) - (4-fluorophenyl) - 3-hydroxypropyl] -4 (S) - (4-hydroxyphenyl) -2-azetidinone (ezetimib) according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI) , (VII), (VIII), (IX), (X), (XI) where the compounds of the general formulas II, IV, VI, VIII, IX, X and XI are new substances, formula III denotes the unselected intermediate product, R1, R2 and R3 are compounds f rmul Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 represents hydrocyanic, e.g. tert-butyldimethylsilyl, tert-butyldiphenylsilyl group. |