A Review of U.S. Patents in the Field of Organic Process Development Published During April and May 2013

摘要

The current review contains 20 from an original list containing 295 that fitted the search criteria. Several of the patents contain an extensive amount of detail such as one describing a process for preparing a quinazoline compound that is of interest in treating cancers. The process involves seven steps that are said to be fewer than those of alternatives. It proceeds via several novel intermediates and includes examples carried out on a kilo scale. Despite this detail, product purities are not reported. Another very extensive patent covers the preparation of prostaglandin analogues and reaction intermediates. The patent describes a novel intermediate that is used to prepare bimatoprost and travoprost. There are several large-scale examples in the patent including one using the reagent K2Os2(OH)4. A key aspect of the patent is that many intermediates do not need to be purified before further use. Another extensive patent describes the preparation of hydroxyalkanamides that are intermediates in the synthesis of hepatitis C drugs.