| 摘要 |
<p>N-Substituted amino acids and dipeptides are valuable intermediates for the preparation of inhibitors of angiotensin converting enzyme (ACE), examples of representatives being enalapril and ramipril. These compounds can be prepared by hydrogenolytic reaction of a primary amine with a ketone, but the known processes are difficult to reproduce and usually still contain considerable amounts of byproducts. The novel process is intended to provide good yields with few byproducts and without additional high costs. The hydrogenolytic reaction is carried out according to the invention with the addition of an organic or inorganic base, with basic aluminium oxide being preferred among the inorganic bases. The formation of one diastereomer is favoured by the use of chiral organic bases. ACE, blood pressure regulators.</p> |
