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US 9,850,198 B2Granted
Process for preparing substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds
AssigneeGruenenthal GmbH
InventorsHelmut Heinrich Buschmann, Joerg Holenz
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Abstract
A process for the preparation of substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds which has advantages over conventional processes with respect to higher conversions and yields, flexibility, a shorter overall route, environmentally acceptable conditions, influence of stereoselectivity such as diastereoselectivity in a targeted manner and at least partial suppression of the formation of undesired side-products and/or undesired stereoisomers, in particular undesired diastereomers.
Claims23
A method of preparing a compound according to formula (I)
- wherein
- R1, R2, and R3 are each independently selected from H or C1-4 aliphatic residues, or a physiologically acceptable acid addition salt thereof, said method comprising the steps of:
- hydrogenating a compound according to formula (C—I)
- wherein R3 is defined above, to a compound a according to formula (C-II)
- wherein R3 is defined as above,
- substituting at least one hydrogen atom of the primary amine group of the compound according to formula (C-II) with a C1-4 aliphatic residue to form the compound according to formula (I), and
- optionally converting the compound according to formula (I) into a physiologically acceptable acid addition salt thereof.
4 more elements
Dependencies are inferred from the claim text.