OBTAINING AND USING PHENYLCYCLOBUTYLAMIDE DERIVATIVES AND STEREOISOMERS THEREOF Russian patent published in 2013 - IPC C07C237/06 A61K31/165 A61P3/04 C07C211/26 

Abstract RU 2479572 C2

FIELD: chemistry.

SUBSTANCE: invention relates to phenylcyclobutylamide derivatives of formula or a stereoisomer or pharmaceutically acceptable salt thereof. In formula (I), R is H, formacyl, acetyl, haloacetyl, benzoyl, benzyloxy carbonyl (Cbz), t-butoxy carbonyl (Boc), or 9-fluorenyl methoxyl carbonyl (Fmoc). The phenylcyclobutylamide derivative of formula (I), where R is H, is used to prepare medicine or a pharmaceutical composition for losing weight. The phenylcyclobutylamide derivatives of formula (I) are obtained by dissolving racemic or separate 1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine and R-protected racemic or D- or L-isoleucine with anhydrous tetrahydrofuran; a condensing agent is then added in droplets to the solution which is then stirred at room temperature overnight, the precipitate is filtered and washed with anhydrous diethyl ether several times. The filtrate and anhydrous diethyl ether eluate are collected; a crude product is the obtained by evaporation, separation and pufification by column chromatography to obtain a racemic or optical isomeric compound, 2-(R-amino)-N-{1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl}-3-methylpentanamide; the R-protection group is removed to obtain a racemic or optical isomeric compound: 2-amino-N-{1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl}-3-methylpentanamide; a pharmaceutically acceptable acid is used to prepare a salt thereof.

EFFECT: phenylcyclobutylamide derivatives which are suitable for treating obesity.

7 cl, 1 tbl, 12 ex

Similar patents RU2479572C2

Title Year Author Number
THERAPEUTIC AGENTS 1998
  • Khil Dehvid
  • Dzhekson Khelen Kristin
RU2234917C2
APPLICATION OF SIBUTRAMINE ANALOGS FOR DECREASING LIPID LEVELS 1997
  • Kelli Piter Finian
  • Dzhons Stefan Pol
RU2197959C2
PHARMACEUTICAL COMPOSITION CONTAINING SIBUTRAMINE AND ORLISTAT 2000
  • Khil Dehvid Dzhon
RU2229289C2
PHARMACEUTICAL COMPOSITION INCLUDING CRYSTALLINE SIBUTRAMINE METHANESULFONATE HEMIHYDRATE 2003
  • Li Dzae-Kheon
  • Park Ga-Seung
  • Li Dzae-Cheol
  • Kim Khan-Kiung
  • Chang Jang-Kil
  • Li Gvan-Sun
RU2290924C2
METHOD OF PRODUCING, METHODS OF USING AND COMPOSITION OF CYCLOALKYLMETHYLAMINES 2007
  • Bkhat Laksminarajjan
  • Bkhat Seema Rani
RU2462451C2
COMPOSITIONS CONTAINING MONOAMINE REUPTAKE INHIBITOR AND METHODS OF THEIR APPLICATION 2004
  • Dzherussi Tomas P.
  • Senanajake Krisanta Kh.
  • Fang Kvun K.
RU2358719C2
COMPOSITIONS COMPRISING INHIBITORS OF DOPAMINE RE-UPTAKE AND METHODS FOR THEIR USING 1999
  • Dzherussi Tomas P.
  • Senanajake Krisanta Kh.
  • Fang Kvun K.
RU2238084C2
COMPOSITIONS, SYNTHESIS AND METHODS FOR APPLICATION OF PHENYLCYCLOALKYLMETHYLAMINE DERIVATIVES 2012
  • Bhat Laxminarayan
  • Adiey Kouacou
  • Bhat Seema Rani
RU2642074C2
APPLICATION OF SIBUTRAMIN ANALOGS FOR PREVENTING DIABETES MELLITUS 1997
  • Behjli Klifford Dzhejms
  • Dzhons Robert Brajn
  • Dzhekson Khelen Kristin
RU2245709C2
(-AMINO-(-HYDROXY-(-ARYLALKANOIC AMIDES AND USE THEREOF AS RENIN INHIBITORS 2004
  • Zell'Ner Khol'Ger
  • Gross Gerkhard
  • Majbaum Jurgen Klaus
  • Kotten Sil'Ven
RU2425027C2

RU 2 479 572 C2

Authors

Zhao Shukjang

Ven Shuming

Ding Khao

Jan Jashi

Chen Ksjaoping

Dates

2013-04-20Published

2009-03-24Filed