Synthesis of phosphaisoquinolin-1-ones by Pd(II)-catalyzed cyclization of o-(1-alkynyl)phenylphosphonamide monoesters |
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Authors: | Tang Wei Ding Yi-Xiang |
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Institution: | Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, Shanghai 200032, China. |
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Abstract: | A Pd(II)-catalyzed intramolecular cyclization of o-(1-alkynyl)phenylphosphonamide monoethyl esters was examined, and a new class of six-membered phosphorus heterocycles (phosphaisoquinolin-1-ones) were formed with high regioselectivity and good yields. The present reaction is the first example of intramolecular addition of P-NH to substituted alkynes, which provides a valuable way to synthesize novel phosphorus heterocycles with potential bioactivities. |
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