1-(Phenylsulfonyl)-5-Methoxy-2-iodo-4-azaindole synthesis

Yield:1206181-42-1 74%

Reaction Conditions:

Stage #1: 1-benzenesulfonyl-5-methoxy-1H-pyrrolo[3,2-b]pyridinewith N,N,N,N,-tetramethylethylenediamine;lithium diisopropyl amide in tetrahydrofuran;n-heptane;ethylbenzene at -78;Inert atmosphere;
Stage #2: with iodine in tetrahydrofuran;n-heptane;ethylbenzene at -78 - 20;Inert atmosphere;regioselective reaction;

References:

Saab, Fabienne;Bénéteau, Valérie;Schoentgen, Fran?oise;Mérour, Jean-Yves;Routier, Sylvain [Tetrahedron,2010,vol. 66,# 1,p. 102 - 110] Location in patent:scheme or table