Process for the preparation of indole derivatives
AssigneeBoehringer Manneheim GmbH
InventorsHelmut Michel, Roland Ofenloch
Life of this patent
Estimating the term…
Loading patent…
AssigneeBoehringer Manneheim GmbH
InventorsHelmut Michel, Roland Ofenloch
Estimating the term…
The present invention provides a process for the preparation of 4-hydroxyindole derivatives of the general formula: ##STR1## in which R.sub.1 is a hydrogen atom or an alkyl radical containing up to 6 carbon atoms and R.sub.2 is a hydrogen atom or an alkyl radical containing up to 6 carbon atoms, wherein a compound of the general formula: ##STR2## in which R.sub.2 has the same meaning as above, is reacted with a compound of the general formula: R.sub.3 --CH.sub.2 --CO--COOR.sub.1 (III) in which R.sub.1 has the same meaning as above and R.sub.3 is a reactive residue, to give a 2-(2-imino-6-oxocyclohexylidene)-propionic acid derivative of the general formula: ##STR3## in which R.sub.1, R.sub.2 and R.sub.3 have the same meanings as above, which is then cyclized in known manner to give a compound of the general formula: ##STR4## in which R.sub.1 and R.sub.2 have the same meaning as above, which is subsequently dehydrated. The present invention also provides new 4-hydroxyindoles of general formula (I'), as well as new 4-Oxo-4,5,6,7-tetrahydroindoles of general formula (IV).
A process for the preparation of a 4-hydroxyindole of the formula:
Dependencies are inferred from the claim text.