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RU96119351A - SEPARATION OF AMLODIPINE ENANTIOMERS THROUGH THEIR DIASTEROMERIC TARTRATES - Google Patents

SEPARATION OF AMLODIPINE ENANTIOMERS THROUGH THEIR DIASTEROMERIC TARTRATES

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Publication number
RU96119351A
RU96119351A RU96119351/04A RU96119351A RU96119351A RU 96119351 A RU96119351 A RU 96119351A RU 96119351/04 A RU96119351/04 A RU 96119351/04A RU 96119351 A RU96119351 A RU 96119351A RU 96119351 A RU96119351 A RU 96119351A
Authority
RU
Russia
Prior art keywords
amlodipine
dmso
solvent
hemi
tartrate
Prior art date
Application number
RU96119351/04A
Other languages
Russian (ru)
Other versions
RU2132845C1 (en
Inventor
Лайонел Спарго Питер
Original Assignee
Пфайзер Рисерч Энд Дивелопмент Компани, Н.В./С.А.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB9405833A external-priority patent/GB9405833D0/en
Application filed by Пфайзер Рисерч Энд Дивелопмент Компани, Н.В./С.А. filed Critical Пфайзер Рисерч Энд Дивелопмент Компани, Н.В./С.А.
Publication of RU96119351A publication Critical patent/RU96119351A/en
Application granted granted Critical
Publication of RU2132845C1 publication Critical patent/RU2132845C1/en

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Claims (13)

1. Способ выделения R-(+)- и S-(-)-изомеров амлодипина из их смесей, заключающийся во взаимодействии смеси изомеров с L- или D-винной кислотой в органическом растворителе, содержащем количество диметилсульфоксида (ДМСО), достаточное для осаждения соответственно ДМСО-сольвата соли L-винной кислоты и R-(+)-амлодипина или ДМСО-сольвата соли D-винной кислоты и S-(-)-амлодипина.1. The method of separation of R - (+) - and S - (-) - isomers of amlodipine from their mixtures, which consists in the interaction of a mixture of isomers with L- or D-tartaric acid in an organic solvent containing enough dimethyl sulfoxide (DMSO) to precipitate respectively, DMSO solvate of a salt of L-tartaric acid and R - (+) - amlodipine or DMSO solvate of a salt of D-tartaric acid and S - (-) - amlodipine. 2. Способ по п.1, отличающийся тем, что растворитель представляет собой ДМСО. 2. The method according to claim 1, characterized in that the solvent is DMSO. 3. Способ по п.1, отличающийся тем, что растворитель представляет собой смесь ДМСО и сорастворителя, причем сорастворитель присутствует в количестве, достаточном для того, чтобы произошло осаждение ДМСО-сольвата. 3. The method according to claim 1, characterized in that the solvent is a mixture of DMSO and a co-solvent, wherein the co-solvent is present in an amount sufficient to precipitate the DMSO solvate. 4. Способ по п.3, отличающийся тем, что сорастворитель представляет собой воду или кетон, спирт, простой эфир, амид, сложный эфир, хлорированный углеводород, нитрил или углеводород. 4. The method according to claim 3, characterized in that the co-solvent is water or ketone, alcohol, ether, amide, ester, chlorinated hydrocarbon, nitrile or hydrocarbon. 5. Способ по п.4, отличающийся тем, что сорастворитель представляет собой воду, ацетон, диметилацетамид, метилэтилкетон, тетрагидрофуран, этилацетат, дихлорметан, диметилформамид, толуол, изопропиловый спирт или N,N'-диметилпропиленмочевину. 5. The method according to claim 4, characterized in that the cosolvent is water, acetone, dimethylacetamide, methyl ethyl ketone, tetrahydrofuran, ethyl acetate, dichloromethane, dimethylformamide, toluene, isopropyl alcohol or N, N'-dimethylpropylene urea. 6. Способ по любому из пп.3-6, отличающийся тем, что сорастворитель присутствует в количестве до 50% по объему в расчете на объем ДМСО. 6. The method according to any one of claims 3 to 6, characterized in that the co-solvent is present in an amount up to 50% by volume based on the volume of DMSO. 7. Способ по п. 6, отличающийся тем, что сорастворитель присутствует в количестве 0,2 - 6% по объему. 7. The method according to p. 6, characterized in that the co-solvent is present in an amount of 0.2 to 6% by volume. 8. Способ по любому из предшествующих пунктов, отличающийся тем, что количество используемой L- или D-винной кислоты составляет около 0,5 моль или около 0,25 моль на моль амлодипина. 8. The method according to any one of the preceding paragraphs, characterized in that the amount of L- or D-tartaric acid used is about 0.5 mol or about 0.25 mol per mol of amlodipine. 9. Способ по любому из предшествующих пунктов, отличающийся тем, что осаждаемый сольват представляет собой соответственно моно-ДМСО-сольват (S)-(-)-амлодипин-геми-D-тартрата или моно-ДМСО-сольват (R)-(+)-амлодипин-геми-L-тартрата. 9. The method according to any one of the preceding paragraphs, characterized in that the deposited solvate is a mono-DMSO solvate (S) - (-) - amlodipine-hemi-D-tartrate or a mono-DMSO solvate (R) - (+ ) -amlodipine-hemi-L-tartrate. 10. Моно-ДМСО-сольват (S)-(-)амлодипин-геми-D-тартрата. 10. Mono-DMSO solvate (S) - (-) amlodipine-hemi-D-tartrate. 11. Моно-ДМСО-сольват (R)-(+)амлодипин-геми-L-тартрата. 11. Mono-DMSO solvate (R) - (+) amlodipine-hemi-L-tartrate. 12. Моногидрат (S)-(-)амлодипин-геми-D-тартрата. 12. Monohydrate (S) - (-) amlodipine-hemi-D-tartrate. 13. Моногидрат (R)-(+)амлодипин-геми-L-тартрата. 13. Monohydrate (R) - (+) amlodipine-hemi-L-tartrate.
RU96119351A 1994-03-24 1995-03-06 Method of isolating r-(+)- and s-(-)-amplodipin isomers from mixtures thereof, (r)-(+) and s-(-)-amplodipin-hemi- l- or d-tartrate solvates and monohydrates RU2132845C1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB9405833.6 1994-03-24
GB9405833A GB9405833D0 (en) 1994-03-24 1994-03-24 Separation of the enantiomers of amlodipine
PCT/EP1995/000847 WO1995025722A1 (en) 1994-03-24 1995-03-06 Separation of the enantiomers of amlodipine via their diastereomeric tartrates

Publications (2)

Publication Number Publication Date
RU96119351A true RU96119351A (en) 1998-12-27
RU2132845C1 RU2132845C1 (en) 1999-07-10

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Application Number Title Priority Date Filing Date
RU96119351A RU2132845C1 (en) 1994-03-24 1995-03-06 Method of isolating r-(+)- and s-(-)-amplodipin isomers from mixtures thereof, (r)-(+) and s-(-)-amplodipin-hemi- l- or d-tartrate solvates and monohydrates

Country Status (27)

Country Link
US (2) US5750707A (en)
EP (1) EP0751938B1 (en)
JP (1) JP2843681B2 (en)
KR (1) KR100188980B1 (en)
CN (1) CN1067055C (en)
AT (1) ATE166050T1 (en)
AU (1) AU677765B2 (en)
BR (1) BR9507137A (en)
CA (1) CA2186263C (en)
CO (1) CO4230248A1 (en)
CZ (1) CZ287324B6 (en)
DE (1) DE69502486T2 (en)
DK (1) DK0751938T3 (en)
ES (1) ES2116737T3 (en)
FI (1) FI113646B (en)
GB (1) GB9405833D0 (en)
HU (1) HU214720B (en)
IL (1) IL113008A (en)
MY (1) MY111979A (en)
NO (1) NO306110B1 (en)
NZ (1) NZ282404A (en)
PE (1) PE48895A1 (en)
PL (1) PL180085B1 (en)
RU (1) RU2132845C1 (en)
TW (1) TW448156B (en)
WO (1) WO1995025722A1 (en)
ZA (1) ZA952362B (en)

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