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US 5,401,854 AGranted
Process for the production of indole derivatives
AssigneeSchering Corporation
InventorsGregor Haffer, Helmut Borner, Wolfgang Kubler, Klaus Nickisch
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Abstract
A process for the production of indole derivatives, which is characterized in that in the presence of phosphoric acid a substitution with an imine is performed, and intermediate products of this process and the production of these intermediate products are described.
Claims13
A process for the production of compounds of formula I ##STR5## wherein R.sup.1 is C.sub.1-4 -alkyl;
- R.sup.4 is hydrogen, C.sub.1-4 -alkyl or C.sub.1-4 -alkoxy-C.sub.1-2 -alkyl;
- and
- R.sup.5 is C.sub.1-4 -alkyl, an optionally substituted phenyl or optionally substituted phenyl-C.sub.2 -alkyl, and --OR.sup.5 can be single or multiple, said process comprising reacting a compound of formula II ##STR6## wherein R.sup.5 has the meaning indicated above, in the presence of phosphoric acids with a compound of formula III
- R.sup.4 --CH.dbd.N--R.sup.1 III,
- wherein R.sup.4 and R.sup.1 have the meanings indicated above.
2 more elements
A compound of formula IIa ##STR7## wherein R.sup.5' is a phenyl mono- or disubstituted by halogen, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, trifluoromethyl, cyano and/or nitro.
Dependencies are inferred from the claim text.