Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1991-01-18
1992-10-20
Springer, David B.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
546178, 548502, C07D20910, C07D40312
Patent
active
051571226
ABSTRACT:
An indole having the formula I: ##STR1## is prepared by a Fischer-Indole reaction employing a mixture of phosphorous pentoxide and methane sulfonic acid as an acid catalyst. The reaction, which is optionally run in a co-solvent, provides 3-unsubstituted indoles in high yields with high regioselectivity. The indole thus prepared is an intermediate in the synthesis of leukotriene biosynthesis inhibitors.
REFERENCES:
P. E. Eaton et al., Phosphorous Pentoxide-Methanesulfonic Acid, J. Org. Chem. 38, 4071 (1973).
A. Guy and J. P. Guette, Utilization of Polyphosphoric Acid Synthesis, 1980, 222.
H. Illy and L. Funderburk, Fisher Indole Syn. Direction of Cyclization, J. Org. Chem., 33, 4283 (1968).
M. H. Palmer and P. S. McIntyre, Fischer Indole Syn. Unsymmetrical Ketones, J. Chem. Soc. (B), 1969, 446.
Hughes David L.
Zhao Dalian
DiPrima Joseph F.
Lopez Gabriel
Merck & Co. , Inc.
Muthard David A.
Springer David B.
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