DERIVATIVES OF 3-ALKYL-5-(4-ALKYL-5-OXOTETRAHYDROFURAN-2-YL)PYRROLIDIN-2-ONE AS INTERMEDIATE COMPOUNDS IN SYNTHESIS OF RENIN INHIBITORS Russian patent published in 2011 - IPC C07D405/04 C07D207/26 C07D307/32 C07F1/02 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula or salts thereof, and compounds of formula or salts thereof, where R³ denotes C₁-C₇alkyl or C₃-C₈cycloalkyl, and R⁴ denotes C₁-C₇alkyl or C₃-C₈cycloalkyl, and Act denotes an activating group selected from an amino protective group, mainly carbamate, as well as methods of producing said compounds. The invention also discloses a method, novel steps of the method and novel intermediate compounds for use in synthesis of pharmaceutically active compounds, mainly renin inhibitors, such as aliskiren. Also, when compounds (VI) react with organometallic compounds (VII) , where Y denotes a metal-containing group such as Li, -MgX, magnesate, aryl-magnesium compound, alkylmagnesium compound, -MnX, (alkyl)₃MnLi- or -CeX₂, where X is a halogen such as Cl, I or Br, more preferably Br, novel compounds are obtained, R³ and R⁴ assume values given for compounds of formula (II), and Act denotes an activating group selected from an amino protective group, mainly carbamate, R¹ denotes a halogen, hydroxyl, halogen(C₁-C₆)alkyl, C₁-C₆alkoxy(C₁-C₆)alkyloxy or C₁-C₆alkoxy(C₁-C₆)alkyl, R² denotes a halogen, hydroxyl, C₁-C₄alkyl or C₁-C₄alkoxy, which are direct precursors for producing aliskiren.

EFFECT: novel compounds and synthesis methods thereof are obtained and described.

61 cl, 13 ex