Chemistry of Heterocyclic Compounds p. 68 - 72 (1985)
Update date:2022-07-29
Topics:
Sycheva, T. V.
Yakhontov, L. N.
A general method was developed for the synthesis of 1,6-disubstituted 4-methyl-5-cyano-7-azaindolines from the readily available ammonium salt of 2,6-dihydroxy-3-(β-hydroxyethyl)-4-methyl-5-cyanopyridine through the corresponding N-substituted ammonium salts and N-substituted 2-amino-3-(β-hydroxyethyl)-4-methyl-5-cyano-6-hydroxypyridines with treatment of the latter by POCl3.This method gives a 40percent yield of 4-methyl-5-cyano-7-azaindoline compounds containing various aralkyl or alkyl substituents at N-1 and a hydroxy group or halogen atom at C-6 in three steps.
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Doi:10.1002/jhet.5570220140
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