The development of anti-hypertensive agents was briefly introduced in this paper, and the mechanisms of Quinapril, the third generation angiotensin converting enzyme inhibitor, was also introduced. The synthesis of Quinapril was studied importantly. A new synthetic route was designed and the process was investigated and improved to make easier, and the yield was elevated. All the work provide the foundation for its industrialization. The total yield was 13.9%, which was synthesized from benzene by eleven steps, including the preparation of side chains. Its structure was confirmed by IR, UV, NMR, elemental analysis, X-ray diffraction analysis.
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