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US 2013/0172572 A1Published application
Process for Manufacture of N-acylbiphenyl alanine
OwnerGuoliang Zhu, Desong Shi +2inventors
InventorsGuoliang Zhu, Desong Shi, Junhui Wei, Fengfeng Tao
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Abstract
A novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.
Claims12
A process for preparing a compound of formula (1-a), or salt thereof,
- preferably wherein the compound of formula (1-a) is of the formula (1),
- wherein R1 is C1-7alkyl, preferably methyl, or C6-10aryl, preferably phenyl,
- comprising
- reacting
- or salt thereof,
- with
- a compound of formula (A), or salt thereof,
- wherein R1 is as defined for the compound of formula (1-a),
- and
- (R2CO)2O, wherein R2 is C1-7alkyl, preferably methyl or propyl,
- under alkaline conditions,
- to provide the compound of formula (1-a).
9 more elements
A process for preparing a compound of formula (2-a), or salt thereof,
- preferably wherein the compound of formula (2-a) is of the formula (2),
- wherein R1 is C1-7alkyl, preferably methyl, or C6-10aryl, preferably phenyl,
- comprising
- reacting
- a compound of formula (1-a), or salt thereof,
- preferably wherein the compound of formula (1-a) is of the formula (1),
- wherein R1 is as defined for a compound of formula (2-a),
- with water
- to provide the compound of formula (2-a).
6 more elements
A process for preparing a compound of formula (3), or salt thereof,
- preferably wherein the compound of formula (3) is of the formula (3-a),
- wherein R1 is C1-7alkyl, preferably methyl, or C6-10aryl, preferably phenyl, comprising
- treating a compound of formula (2-a), or salt thereof,
- preferably wherein the compound of formula (2-a) is of the formula (2),
- wherein R1 is C1-7alkyl, preferably methyl, or C6-10aryl, preferably phenyl,
- under hydrogenation conditions
- to provide the compound of formula (3).
4 more elements
A compound of formula (1-a), or salt thereof,
- preferably wherein the compound of formula (1-a) is of the formula (1),
- wherein R1 is C1-7alkyl, preferably methyl, or C6-10aryl, preferably phenyl.
A compound of formula (2-a), or salt thereof,
- preferably wherein the compound of formula (2-a) is of the formula (2),
- wherein R1 is C1-7alkyl, preferably methyl, or C6-10aryl, preferably phenyl.
A compound of formula (3), or salt thereof,
- preferably wherein the compound of formula (3) is of the formula (3-a),
- wherein R1 is C1-7alkyl, preferably methyl, or C6-10aryl, preferably phenyl.
Dependencies are inferred from the claim text.