| 摘要 |
The present invention provides a novel, industrially easily realizable and economical process comprising only few steps and built on the use of the new intermediates for the production of 1-(4-3(R)-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe), according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI), wherein the compounds of the general formulas II, IV, VI, VIII, IX, X and XI are the new substances, formula III is a non-isolated intermediate, R1, R2 and R3 are represented by the compounds of formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silil, e.g. tert-buthyl-dimethyl-silil, tert-buthyl-diphenyl-silil group. |
