RESUMO
The approach of utilizing protecting groups (PGs) in organic chemistry has led to the successful syntheses of an array of useful organic compounds. This strategy has also addressed some of the complexities associated with many organic reactions. These PGs find useful applications in simple and complex reactions that involve the synthesis of large organic compounds such as peptides, and oligosaccharides. The fundamental role of PGs is to prevent undesired reactions that could hinder the progress or completion of such reactions. Ideal PGs must be utilized in this regard to achieve the desired objectives. This review describes the diverse protecting groups found in the literatures, the functional moieties for the protection, deprotection strategies, and their relevant applications in organic synthesis.
RESUMO
BACKGROUND: Entrectinib is a highly potent ATP-competitive and selective inhibitor of tyrosine kinases - Trk A B C, ALK, and ROS1. It was developed by Roche and initially approved in Japan in 2019 to treat pediatric and adult patients with NTRK fusionpositive, recurrent, or advanced solid tumors. In August 2019, entrectinib received accelerated approval by the U.S FDA for this indication. It is also the first FDA-approved drug designed to target both NTRK and ROS1. OBJECTIVE: We aim to summarize recent studies related to the synthesis, mechanism of action, and clinical trials of the newly approved selective tyrosine kinase inhibitor entrectinib. METHODS: We conduct a literature review of the research studies on the new highly-potent small-molecule entrectinib. CONCLUSION: Entrectinib, based on three clinical studies (ALKA, STARTRK-1, and STARTRK-2), was well tolerated, with a manageable safety profile. It induced clinically meaningful responses in recurrent or advanced solid tumors associated with NTRK fusion- positive or ROS1+ NSCLC. It demonstrated substantial efficacy in patients with CNS metastases.