A scalable total synthesis of Et-743 and lurbinectedin.

An efficient and scalable approach for total synthesis of Et-743 and lubinectedin (about 1.6% overall yield in 26 total steps from Cbz-protected (S)-tyrosine) is described, and features the use of a common advanced intermediate to create the right and left parts of these antitumor drugs, and a light-mediated remote C-H bond activation to assemble a benzo[1,3]dioxole-embodied intermediate.