Novartis Ag

Bial-portela Ca & S.a.

Novartis Pharmaceuticals Corporation

Jonathan Medlock

Antonio Zanotti-Gerosa

David Hook

Daniel Kaufmann

Erhard Bappert

Matthias Napp

Philippe Polleux

Bernard Riss

Gabriela Alexandra Grasa

Beatriz Dominguez

Bernhard Riss

The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a &#x3b3;-amino-&#x3b4;-biphenyl-&#x3b1;-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.

Intermediates for producing NEP inhibitors or prodrugs thereof

Processes for producing NEP inhibitors or prodrugs thereof

A diamine of formula (I) is described in which A is hydrogen or a saturated or unsaturated C1-C20 alkyl group or an aryl group; B is a substituted or unsubstituted C1-C20 alkyl, cycloalkyl, alkaryl, alkaryl or aryl group or an alkylamino group and at least one of X, X, Y, Yor Z is a C1-C10 alkyl, cycloalkyl, alkaryl, aralkyl or alkoxy substituting group. The chiral diamine may be used to prepare catalysts suitable for use in transfer hydrogenation reactions. 

Sulphonylated diphenylethylenediamines, method for their preparation and use in transfer hydrogenation catalysis

Processes

A diamine of formula (I) is described, in which A is hydrogen or a saturated or unsaturated C1-C20 alkyl group or an aryl group; B is a substituted or unsubstituted C1-C20 alkyl, cycloalkyl, alkaryl, alkaryl or aryl group or an alkylamino group and at least one of X, X, Y, Yor Z is a C1-C10 alkyl, cycloalkyl, alkaryl, aralkyl or alkoxy substituting group. The chiral diamine may be used to prepare catalysts suitable for use in transfer hydrogenation reactions. 

Growing community of inventors

Cambridge, United Kingdom

Jonathan Medlock