ChemInform Abstract: Expeditious Synthesis of Ramipril: An Angiotensin-Converting Enzyme (ACE) Inhibitor

We document an efficient and cost‐effective synthesis of ramipril 1 utilizing (i) an environmentally benign process for the esterification of racemic 2‐aza‐bicyclo‐[3.3.0]‐octane‐3‐carboxylic acid hydrochloride 2 using boric acid as a catalyst and (ii) a robust resolution process for the synthesis of 3a by means of inexpensive and recyclable L‐(+)‐mandelic acid as key steps.