- Preparation method of (R)-2-(N-tertbutyloxycarbonylamino)biphenylpropanol
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The invention discloses a preparation method of (R)-2-(N-tertbutyloxycarbonylamino)biphenylpropanol represented by formula (I). The method comprises the following steps: carrying out an Erlenmeyer-Plochl cyclization reaction on biphenylcarboxaldehyde and N-acylglycine, hydrolyzing or alcoholyzing, and carrying out asymmetric hydrogenation to obtain (R)-N-acylbiphenylalanine or an ester thereof; and carrying out acid hydrolysis, reduction and amino protection on the (R)-N-acylbiphenylalanine or the ester thereof, or carrying out reduction, acid hydrolysis and amino protection on the (R)-N-acylbiphenylalanine or the ester thereof, or directly reducing the (R)-N-acylbiphenylalanine or the ester thereof in order to obtain the product (R)-2-(N-tertbutyloxycarbonylamino)biphenylpropanol. The product is a key intermediate of Sacubitril (AHU-377) which is one of a novel blood pressure reducing medicine LCZ696. The method has the advantages of easily available raw materials, and suitableness for industrial production.
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- NEW PROCESS
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The invention relates to a new enantioselective process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone.
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- NEW PROCESS
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Provided is a new enantioselective process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ -amino- δ -biphenyl- a -methylalkanoic acid, or acid ester, backbone.
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