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US 6,274,735 B1Granted
Process and intermediates for preparation of substituted piperidines
AssigneeHoffmann-La Roche Inc.
InventorsBruno Lohri, Rudolf Schmid, Eric Vieira
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Abstract
The present invention concerns intermediates useful in and a process for the preparation of a compound of formula 1 or a salt thereof comprising a) hydroboration of a compound of formula 2 A, R1 and R2 are as herein defined. These compounds are useful in the synthesis of renin inhibitors.
Claims16
A compound having the formula
- wherein
- A is arylene;
- R1 is —C*R3R4R5;
- R2 is —O-alkyl, —O-cycloalkyl, —O-alkenyl, —O-aryl, —O-aralkyl, —O-aralkoxyalkyl, —O-alkylsulfonyl, —O-arylsulfonyl;
- R3 is hydrogen;
- R4 is aryl;
- R5 is alkyl, cycloalkyl, aryl, alkoxyalkyl or hydroxyalkyl;
- and
- C* is an asymmetric carbon atom;
- and
- salts of said compound.
8 more elements
A process for the preparation of a compound of formula 1, or a salt thereof,
- comprising:
- a) hydroboration of a compound of formula 2
- wherein,
- A is arylene;
- R1 is —C*R3R4R5;
- R2 is —O-alkyl, —O-cycloalkyl, —O-alkenyl, —O-aryl, —O-aralkyl, —O-aralkoxyalkyl, —O-alkylsulfonyl, —O-arylsulfonyl;
- R3 is hydrogen;
- R4 is aryl;
- R5 is alkyl, cycloalkyl, aryl, alkoxyalkyl or hydroxyalkyl;
- and
- C* is an asymmetric carbon atom.
8 more elements
Dependencies are inferred from the claim text.