Process for preparing 5-aza-indole and intermediates used in thi

Details Process for preparing 5-aza-indole and intermediates used in thi Process for preparing 5-aza-indole and intermediates used in thi

1985-05-28

1986-11-25

Jiles, Henry R.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546329, 546193, 546281, 546312, 544124, C07D47104, C07D21338

Patent

active

046250336

ABSTRACT:
A process for preparing 1H-pyrrolo-[3,2-c]-pyridine or 5-aza-indole in high yield, comprising condensing 3-methyl-4-nitropyridine-1-oxide with a compound having a formula ##STR1## wherein R represents a di-loweralkylamino, morpholino, piperidino or pyrrolidino group and R.sub.1 and R.sub.2, which are the same or different, each represent a loweralkoxy group or a group R as defined; to form an enamine having a formula: ##STR2## wherein R is as define and subjecting the enamine IV to reduction cyclization; the enamines IV are new compounds.

REFERENCES:
Journal of Medicinal Chemistry, vol. 14, No. 11, Nov. 1972, pp. 1168-1171, Washington, D.C.
Chemical Abstracts, vol. 87, No. 25, Dec. 19, 1977, p. 714, "Synthesis of 6-Azaindole".
Khim. Geterotsikl. Soedin., 1977, (8), 1135-6.
Synthesis of 4-Azaindoles, Azimov et al.

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