FIELD: chemistry.
SUBSTANCE: invention relates to a single-step method of producing a compound of formula (III), wherein R1 represents (C1-C7)alkyl or substituted or unsubstituted (C6-C10)aryl, such as phenyl or para-chlorophenyl. The method involves converting a compound of formula (IV) into a compound for formula (II) while heating in the presence or absence of a solvent. The invention also relates to chiral compound of formula (II), a method for production thereof, which involves reaction of a compound of formula (III) with a chiral amine of formula (V) and separation the obtained mixture of diastereomers via crystallisation, and use of said compound in synthesis of a neutral endopeptidase (NEP) inhibitor or prodrug thereof, which includes γ-amino-δ-biphenyl-α-methylcarboxylic acid or acid ester as a supporting structure. The invention also discloses alternative methods of producing a compound of formula (I), involving treating a compound of formula (II) with an acid reagent.
EFFECT: novel intermediate compounds and novel methods of producing compounds used in synthesis of NEP inhibitors.
23 cl, 4 dwg, 34 ex
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Authors
Dates
2014-06-20—Published
2010-01-12—Filed