A Review of U.S. Patents in the Field of Organic Process Development Published During June and July 2011

摘要

The current review contains 19 patents from an original list containing 267 that fitted the selection criteria. This is slightly fewer than usual although several of the patents reviewed cover a considerable volume of process chemistry. A notable feature in several of the current collection is the lack of analytical detail or reaction yield information. It is quite unacceptable that many patents omit vital process information such as the yield of a reaction and even details regarding its purity or method of analysis. If this information was omitted from papers submitted for publication in the open literature, it is expected that they would be rejected. At the very least, these details would be submitted as Supporting Information. It is a fact of life that patents claims can be excessive, but at the least, some evidence for them should be presented. As an example, an extensive patent reports on the synthesis of an intermediate used to make a drug for treating diabetes. The patent does not contain physical property data apart from the bp of those compounds recovered by distillation. Treatments for inflammatory diseases have a large market and are of great value; a process to prepare individual stereoisomers of arylcyclopentane carboxylates is described. The patent contains a large amount of detailed chemistry, but process yields are low.