Asymmetric Synthesis of a Prostaglandin D_2 Receptor Antagonist

摘要

An asymmetric synthesis was developed for the production of a prostaglandin D_2 receptor antagonist for the treatment of allergic rhinitis.The stereogenicr center was set using asymmetric allylic alkylation chemistry,and the core of the structure was constructed via Pd-catalyzed N-cyclization/ Heck methodology.The synthesis relies on a late stage indoline oxidation which does not racemize the product.