METHOD FOR OBTAINING 5-CHLORO-N-(5S)-2-OXO-3-[4-(3-OXO-MORPHOLINYL)-PHENYL]-1,3-OXAZOLIDIN-5-YL}-METHYL)-2-THIOPHENECARBOXAMIDE IN MODIFICATION II (VERSIONS) Russian patent published in 2016 - IPC C07D413/14 A61K31/5377 A61P7/02 

Abstract RU 2578602 C2

FIELD: chemistry.

SUBSTANCE: invention relates to method for obtaining 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide, represented by formula

,

in modification II (thereof versions). Method for obtaining formula (I) in modification II, characterised by the following spectral data in nearest IR region [cm-1]: 4086, 4228, 4418, 4457, 4634, 4905, 5846, 5911, 6026, 6081, 6582, consists in the fact that compound of formula (I) in modification I, characterised by the following spectral data in nearest IR region [cm-1]: 4082, 4142, 4170, 4228, 4299, 4376, 4429, 4479, 4633, 4791, 4877, 4907, 5081, 5760, 5885, 6002, 6441, 6564, 8473, 8833, is dissolved in inert solvent, selected from the group, including acetone, tetrahydrofuran, 1-pentanol and their mixtures, and compound is precipitated by addition of n-heptane additive at temperatures within from 0 to 80°C. Method for obtaining compound of formula (I) in modification II, is also realised by dissolution of compound (I) in modification I in 1,4-dioxane, with exposure of solution at temperature within from 30°C to temperature of solvent reflux till complete solvent evaporation. Method for obtaining compound of formula (I) in modification II is realised by suspending compound (I) in modification I in ethanol with mixing or shaking suspension at temperature within from 20 to 25°C until transformation into modification II occurs.

EFFECT: obtaining 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide, represented by formula

,

in modification II, possessing high solubility.

4 cl, 12 dwg, 7 tbl, 2 ex

Similar patents RU2578602C2

Title Year Author Number
NOVEL POLYMORPHOUS FORM AND AMORPHOUS FORM OF 5-CHLORO-N-({(5S)-2-OXO-3-[4-(3-OXO-4-MORPHOLINYL)-PHENYL]-1,3-OXAZOLIDIN-5-YL}-METHYL)-2-THIOPHENE CARBOXAMIDE 2006
  • Grunenberg Al'Fons
  • Lents Jana
  • Braun Gerkhard Arnol'D
  • Kajl' Birgit
  • Tomas Kristian R.
RU2429236C2
METHOD FOR SYNTHESIS OF 5-CHLORO-N-({(5S)-2-OXO-3-[4-(3-OXO-4-MORPHOLINYL)-PHENYL]-1,3-OXAZOLIDIN-5-YL}-METHYL)-2-THIOPHENECARBOXAMIDE 2004
  • Berve Matias
  • Tomas Kristian
  • Reze Joakhim
  • Grotjokhann Dirk
RU2383540C2
NOVEL CRYSTALLINE FORM OF 5-CHLORO-N-({(5S)-2-OXO-3-[4-(5,6-DIHYDRO-4H-[1,2,4]TRIAZIN-1-YL)PHENYL]-1,3-OXAZOLIDIN-5-YL}METHYL)THIOPHENE-2-CARBOXAMIDE METHANESULPHONATE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME 2014
  • Choj Soongiu
  • Choj Dzungsub
  • Joon So-Khiun
  • Kim Joo Khoon
  • Kim Dzae Jeon
  • Li Suk Kho
  • Cho Joung Lag
  • Song Kho Joung
  • Li Dae Jon
  • Baek Sung Joon
  • Chae Sang Eun
  • Park Tae Kio
  • Voo Sung Kho
  • Kim Jong Zu
RU2663617C1
ORAL SOLID PHARMACEUTICAL FORMS WITH FAST RELEASE ACTIVE SUBSTANCE 2006
  • Benke Klaus
RU2440119C2
COMBINED THERAPY USING SUBSTITUTED OXAZOLIDINONES 2002
  • Shtraub Aleksander
  • Lampe Tomas
  • Pernershtorfer Dzhozef
  • Pertsborn Ehlizabet
  • Pol'Mann Jens
  • Rerig Sjuzanne
  • Shlemmer Karl-Khajnts
RU2321407C9
ANTIBIOTIC DERIVATIVES OF 2-OXO-OXAZOLIDINE-3, 5-DIYL 2012
  • Khubshverlen Kristian
  • Ryuedi Georg
  • Syurive Zhan-Filipp
  • Tsumbrunn-Aklen Korneliya
RU2616609C2
TARTARE SALT [(S)-2-[METHYL-3-(2-OXO-PYRROLIDIN-1-YL)- BENZENESULFONYLAMINO]-3-(4-METHYL-PIPERAZINE-1-YL)-3-OXO-PROPYL]AMIDE 5-CHLORINE-THIOPHENE-2- CARBOXYLIC ACID 2014
  • Lyafferrer Loran
  • Vijon Sebasten
  • Gote Sandrin
  • Burbon Andre
RU2664538C2
SUBSTITUTED OXAZOLIDINONES, METHODS FOR THEIR PREPARING, MEDICINAL AGENT BASED ON THEREOF AND USING SUBSTITUTED OXAZOLIDINONES 2000
  • Shtraub Aleksandr
  • Lampeh Tomas
  • Pol'Mann Jens
  • Rerig Zuzan
  • Pertsborn Ehlizabet
  • Shlemmer Karl-Khajnts
  • Pernershtorfer Jozef
RU2297415C2
4-HYDROXYBENZOPYRAN-2-ONE OR 4-HYDROXYCYCLOALKYL[B]BENZOPYRAN- -2-ONE AND, METHOD OF SYNTHESIS OF N-[3-[CYCLOPROPYL- -(5,6,7,8,9,10-HEXAHYDRO-4-HYDROXY-2-OXO-2H-CYCLOOCTA[B]- -PYRAN-3-YL)METHYL]PHENYL]-BENZENESULFONE 1994
  • Dehvid Dzhon Anderson
  • Li S.Behnitt
  • Pol Kosta Tomich
  • Majkl Dzhon Bokhehnon
  • Stiven Ronal'D Terner
  • Dzhozef Val'Ter Shtrobakh
  • Suvit Taisrivongs
  • Ching-Ping Jang
  • Richard S.Tomas
  • Karen Ren Romines
  • Pol Adrian Aristoff
  • Kharvej Irving Skul'Nik
  • Pol D.Dzhonson
  • Ronal'D V.Gehmmill
  • Kvingvej Zang
  • Gordon L.Bandi
RU2125999C1
3-AMINOALKYL-1,4-DIAZEPAN-2-ONE MELANOCORTIN-5 RECEPTOR ANTAGONISTS 2009
  • Blaskovich Mark Arnol'D Tomas
  • Kehssidi Piter Dzhozef
RU2530017C2

RU 2 578 602 C2

Authors

Grunenberg Alfons

Lents Jana

Braun Gerkhard Arnold

Kajl Birgit

Tomas Kristian

Dates

2016-03-27Published

2006-09-22Filed