Development of a Practical and Efficient Synthesis
of SIPI-4884, a HMG CoA Reductase Inhibitor for the Treatment of Hypercholesterolemia
- Publication date
- Publisher
Abstract
An
improved process of the novel HMG CoA reductase inhibitor SIPI-4884
has been developed for early preclinical pharmacology and safety studies,
and it was made up with an efficient nine-step and scalable process.
Significant improvements in the nucleophilic substitution, reduction,
Wittig–Horner reaction, and preparation of calcium salt were
demonstrated. The overall yield was improved to 17.2%