A straightforward, mild, additive-free, and catalyst-free method for the phosphorylation of indolyl-containing quaternary phosphonium salts with phosphine oxides has been developed. This process involves a formal C-+P to C-P(O) bond exchange, encompassing the cleavage of a C-+P bond and the formation of a C-P(O) bond. Through this method, a variety of structurally diverse and potentially bioactive 3-(phosphoryl)methylindoles were synthesized in moderate to good yields with good functional group tolerance. Furthermore, the protocol exhibits excellent scalability and facilitates the easy transformation of the resulting products.
Ji et al. (Thu,) studied this question.