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 

Abstract RU 2432354 C2

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

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RU 2 432 354 C2

Authors

Zedel'Majer Gottfrid

Grimle Dominik

Adzhemoglu Murat

Dates

2011-10-27Published

2006-10-16Filed