摘要 |
<p>A process is provided for preparing (trans)-4-phenyl-L-proline derivatives, which are useful in preparing certain angiotensin converting enzyme inhibitors, which process involves Friedel-Crafts alkylation of benzene with a proline derivative wherein a proline derivative of the structure <IMG> or a proline lactone of the structure <IMG> wherein R is a nitrogen protecting group, R1 is H, aryl, arylalkyl or lower alkyl, and X is a leaving group such as fluorine or mesyl, is reacted with benzene in the presence of a Lewis acid such as AlCl3 to form the (trans)-4-phenyl-L-proline derivative of the structure <IMG> wherein R1 must be H where the proline starting material is employed.</p> |