Synthetic Approaches for Pharmacologically Active Decorated Six-Membered Diazines

The document "Synthetic Approaches for Pharmacologically Active Decorated Six-Membered Diazines" discusses the pharmacological applications and synthesis methods of diazine alkaloids, particularly pyrimidines. These compounds exhibit various biological activities and are used in many therapeutic disciplines, including treatment for myeloid leukemia, breast cancer, idiopathic pulmonary fibrosis, and hair disorders. The document details the synthesis of four FDA-approved drugs: Pazopanib, Spebrutinib, Dabrafenib, and Rilpivirine, and provides detailed synthetic processes for each. It also proposes an alternative six-step process for synthesizing Rilpivirine, which improved the yield of the final amination product from 69% to 71%. The synthesis of Minoxidil, a drug used to promote hair regrowth and treat androgenetic alopecia, is also discussed, with a two-step procedure yielding an 80% yield and high purity. The document emphasizes the importance of the order and type of linkage between substituents and the heterocyclic pyrimidine in determining the final product.