Crixivan Intro

CRIXIVAN (Indinavir Sulfate) is an orally active HIV protease inhibitor that serves as an excellent example of complex organic synthesis. The molecule contains five stereogenic centers, leading to 2⁵ or 32 potential stereoisomers, yet only a single pure enantiomer is required. The synthesis employs a convergent strategy, using a three-carbon linker to connect the 'western' piperazine fragment to the 'eastern' indanolamide fragment. This method has proven highly effective on a multi-ton scale, necessary for production. Careful control is essential to avoid forming diastereomers, requiring each fragment to be synthesized in a nonracemic form.