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
Title | Year | Author | Number |
---|---|---|---|
METHOD FOR PREPARING HERBICIDE DERIVATIVES AND INTERMEDIATE COMPOUND | 2000 |
|
RU2244715C2 |
ALTERNATIVE METHODS FOR SYNTHESIS OF RENIN INHIBITORS AND INTERMEDIATE COMPOUNDS THEREOF | 2005 |
|
RU2411230C2 |
LIQUID FORMULATIONS | 2006 |
|
RU2470631C2 |
LIQUID COMPOSITIONS | 2006 |
|
RU2428180C2 |
METHOD OF 4-HYDROXYPROLINE SUBSTRUCTURE-CONTAINING COMPOUND SYNTHESIS | 2003 |
|
RU2392265C2 |
3,5-SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS | 2006 |
|
RU2415840C2 |
USING SIP RECEPTOR MODULATORS IN OPHTHALMOLOGY | 2006 |
|
RU2497513C2 |
S1P RECEPTOR MODULATORS FOR MULTIPLE SCLEROSIS TREATMENT | 2007 |
|
RU2617502C2 |
SIP RECEPTOR MODULATORS FOR TREATING MULTIPLE SCLEROSIS | 2007 |
|
RU2495664C2 |
MODULATORS OF RECEPTOR S1P FOR TREATMENT OF MULTIPLE SCLEROSIS | 2007 |
|
RU2569732C9 |
Authors
Dates
2011-10-27—Published
2006-10-16—Filed