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US 7,598,399 B2Granted
Methods for synthesis of 3-amino-1-arylpropyl indoles
AssigneeRoche Palo Alto LLC
InventorsTerrence Joseph Connolly, Robert P. Farrell, Eric Roy Humphreys, Stephen M. Lynch, Keshab Sarma
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Abstract
A method comprising: hydrogenating an indole propionamide compound of formula h with vitride, to form an aminopropyl indole compound of formula i wherein m, Ar, R1 and R2 are as defined herein. The compounds prepared by the method of the invention are useful as monoamine reuptake inhibitors useful for treatment of CNS indications.
Claims15
A method for preparing a compound of formula i:
- wherein:
- m is from 0 to 4;
- Ar is optionally substituted aryl or optionally substituted heteroaryl;
- each R1 is independently alkoxy, cyano, alkyl, halo, —S(O)rRa;
- or —C(═O)NRbRc wherein r is an integer from 0 to 2, and each of Ra, Rb, and Rc is independently hydrogen or alkyl;
- and
- R2 is alkyl;
- the method comprising hydrogenating an indole propionamide compound of formula h
- with vitride, to form the aminopropyl indole compound of formula i.
6 more elements
Dependencies are inferred from the claim text.