Process Development of an Efficient and Cost-Effective Telescoping Route to a Key Synthetic Precursor for the Preparation of a Renin Inhibitor

Here, we describe an efficient and cost-effective telescoping route to the pharmacologically active form (2), which is a key manufacturing precursor to a novel renin inhibitor for the treatment of hypertension. An efficient synthetic route to the target compound was established with 64% overall yield over nine steps with three isolations.