Synthesis 2022; 54(07): 1823-1832
DOI: 10.1055/s-0040-1720922
paper

4-Alkyl-3-azidomethyl-2-ethoxy-2,5-dihydro-5H-1,2-oxaphosphole 2-Oxides: Synthesis and 1,3-Cycloaddition

Valery K. Brel
,
Ekaterina P. Alekseychuk
,
Oleg I. Artyushin
,
Lada V. Anikina


Abstract

Starting from phosphorylated allenes, a three-steps synthesis of a new class of organic azides with a 1,2-oxaphospholene carbon skeleton has been developed. The series of obtained 4-alkyl-3-azidomethyl-2-ethoxy-2,5-dihydro-5H-1,2-oxaphosphole 2-oxides were utilized in the 1,3-cycloaddition with alkyl 2-[1-(propyn-2-yl)-1H-indol-3-yl]-2-oxoacetates for the synthesis of conjugates, which are potentially active cytostatics.

Supporting Information



Publikationsverlauf

Eingereicht: 18. Juni 2021

Angenommen nach Revision: 17. September 2021

Artikel online veröffentlicht:
21. Oktober 2021

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