Carl A. Busacca

TL;DR: In this article, a number of selected, noteworthy industrial examples are discussed to showcase the catalytic technologies that have been successfully practiced on large scales for active pharmaceutical ingredient (API) synthesis.

TL;DR: The new BIPI ligands are phosphinoimidazolines that can be electronically tuned in three different ligand regions to explore electronic effects in asymmetric catalysis and their application to the asymmetric Heck reaction in the creation of a chiral quaternary center is described.

TL;DR: A Cu-catalyzed coupling of sodium thiosulfate with aryl and vinyl halides was developed to access S-aryl and S-vinyl Bunte salts, and this route to sulfides avoids the use of malodorous thiol starting materials or byproducts.

TL;DR: DIBAL-H and triisobutylaluminum hydride have been found to be outstanding reductants for secondary phosphine oxides (SPOs), and many SPOs can now be reduced at cryogenic temperatures, and conditions for preservation of reducible functional groups have be found.

TL;DR: Dramatic improvement of the key RCM reaction in the synthesis of HCV protease inhibitor BILN2061 can be achieved by N-substitution of the diene substrate with an electron-withdrawing group, and theoretical evidence that such modification may also increase the thermodynamic preference of the macrocyclic product over the dienes substrate is provided.