RU97112881A - METHOD OF OBTAINING LAMOTRIGIN - Google Patents

METHOD OF OBTAINING LAMOTRIGIN

Info

Publication number
RU97112881A
RU97112881A RU97112881/04A RU97112881A RU97112881A RU 97112881 A RU97112881 A RU 97112881A RU 97112881/04 A RU97112881/04 A RU 97112881/04A RU 97112881 A RU97112881 A RU 97112881A RU 97112881 A RU97112881 A RU 97112881A
Authority
RU
Russia
Prior art keywords
formula
lamotrigine
compound
salt
obtaining
Prior art date
Application number
RU97112881/04A
Other languages
Russian (ru)
Other versions
RU2145602C1 (en
Inventor
Реймонд Джеффри Уинтер
Дейвид Алан Сойер
Эндрью Джермейн
Original Assignee
Де Вэллкам Фаундейшн Лимитед
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 GB9426439A external-priority patent/GB9426439D0/en
Priority claimed from GB9426447A external-priority patent/GB9426447D0/en
Application filed by Де Вэллкам Фаундейшн Лимитед filed Critical Де Вэллкам Фаундейшн Лимитед
Priority claimed from PCT/GB1995/003048 external-priority patent/WO1996020934A1/en
Publication of RU97112881A publication Critical patent/RU97112881A/en
Application granted granted Critical
Publication of RU2145602C1 publication Critical patent/RU2145602C1/en

Links

Claims (1)

1. Способ получения ламотригина формулы I
Figure 00000001

при котором соединение формулы II
Figure 00000002

где R представляет собой CN или CONH2,
в органическом растворителе подвергают облучению ультрафиолетовым или видимым светом, а, если R представляет собой CN, то нагреванию.1. The method of obtaining lamotrigine formula I
Figure 00000001

wherein the compound of formula II
Figure 00000002

where R represents CN or CONH 2 ,
in an organic solvent, is irradiated with ultraviolet or visible light, and, if R is CN, then heated. 2. Способ по п. 1, отличающийся тем, что соединение формулы II облучают при кипячении с обратным холодильником в пропан-1-оле. 2. The method according to p. 1, characterized in that the compound of formula II is irradiated by boiling under reflux in propan-1-ole. 3. Способ по п. 1 или 2, отличающийся тем, что соединение формулы II, в которой R представляет собой CN, получают дегидратацией соединения формулы III
Figure 00000003

4. Способ по п. 1 или 2, отличающийся тем, что соединение формулы II, в которой R представляет собой CONH2, получают обработкой 2,3-дихлорфенилглиоксиламида формулы VIII
Figure 00000004

аминогуанидином или его солью.3. The method according to p. 1 or 2, characterized in that the compound of formula II, in which R is a CN, is obtained by dehydration of the compounds of formula III
Figure 00000003

4. The method according to p. 1 or 2, characterized in that the compound of formula II, in which R is a CONH 2 , is obtained by treatment of 2,3-dichlorophenylglyoxylamide formula VIII
Figure 00000004

aminoguanidine or its salt. 5. Способ по любому из пп. 1-4, отличающийся тем, что ламотригин дополнительно превращают в фармацевтически приемлемую соль, полученную присоединением кислоты. 5. A method according to any one of claims. 1-4, characterized in that the lamotrigine is additionally converted into a pharmaceutically acceptable salt obtained by addition of an acid. 6. Способ по п. 5, отличающийся тем, что указанная соль является изетионатом ламотригина. 6. The method according to p. 5, characterized in that the salt is lamotrigine isetionate. 7. Способ по любому из пп. 1-6, отличающийся тем, что ламотригин или его соль, полученную присоединением кислоты, дополнительно смешивают с фармацевтически приемлемым носителем или разбавителем с получением фармацевтической композиции. 7. A method according to any one of claims. 1-6, characterized in that the lamotrigine or its salt obtained by the addition of an acid, further mixed with a pharmaceutically acceptable carrier or diluent to obtain a pharmaceutical composition. 8. Аминогуанидоноксим формулы III
Figure 00000005

9. 2,3-дихлорфенилглиоксиламид формулы V
Figure 00000006

10. Этил-2,3-дихлорфенилглиоксилат формулы VI
Figure 00000007
8. Aminoguanidonoxime formula III
Figure 00000005

9. 2,3-dichlorophenylglyoxylamide formula V
Figure 00000006

10. Ethyl 2,3-dichlorophenylglyoxylate of formula VI
Figure 00000007
RU97112881A 1994-12-30 1995-12-29 Method of lamotrigine producing, intermediate compounds and method of pharmaceutical composition preparing RU2145602C1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB9426447.0 1994-12-30
GB9426439A GB9426439D0 (en) 1994-12-30 1994-12-30 Process
GB9426447A GB9426447D0 (en) 1994-12-30 1994-12-30 Process
GB9426439.7 1994-12-30
PCT/GB1995/003048 WO1996020934A1 (en) 1994-12-30 1995-12-29 Process for the preparation of lamotrigine

Publications (2)

Publication Number Publication Date
RU97112881A true RU97112881A (en) 1999-05-27
RU2145602C1 RU2145602C1 (en) 2000-02-20

Family

ID=26306284

Family Applications (1)

Application Number Title Priority Date Filing Date
RU97112881A RU2145602C1 (en) 1994-12-30 1995-12-29 Method of lamotrigine producing, intermediate compounds and method of pharmaceutical composition preparing

Country Status (13)

Country Link
US (1) US5912345A (en)
EP (1) EP0800520B1 (en)
JP (1) JPH11501007A (en)
AT (1) ATE219487T1 (en)
AU (1) AU4311596A (en)
DE (1) DE69527153T2 (en)
DK (1) DK0800520T3 (en)
ES (1) ES2177672T3 (en)
FI (1) FI972719A (en)
HU (1) HU224688B1 (en)
PT (1) PT800520E (en)
RU (1) RU2145602C1 (en)
WO (1) WO1996020934A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6420354B1 (en) 1998-06-08 2002-07-16 Advanced Medicine, Inc. Sodium channel drugs and uses
GB9812413D0 (en) * 1998-06-10 1998-08-05 Glaxo Group Ltd Compound and its use
US6479498B1 (en) 1999-06-04 2002-11-12 Theravance, Inc. Sodium channel drugs and uses
AU763244B2 (en) * 2000-01-03 2003-07-17 Rpg Life Sciences Limited A process for the preparation of 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine, commonly known as lamotrigine
DE10134980C2 (en) 2001-07-17 2003-05-28 Helm Ag Process for the preparation of lamotrigine
CA2366521C (en) 2001-12-24 2007-03-06 Brantford Chemicals Inc. A new and efficient process for the preparation of lamotrigine and related 3,5-diamino-6-substituted-1,2,4-triazines
HU225667B1 (en) 2002-09-20 2007-05-29 Richter Gedeon Nyrt Method for producing high-purity 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine
US20120142919A1 (en) * 2006-08-02 2012-06-07 Medichem, S.A. Method for synthesizing lamotrigine
WO2009061513A1 (en) * 2007-11-09 2009-05-14 Thar Pharmaceuticals Crystalline forms of lamotrigine

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3637688A (en) * 1970-01-09 1972-01-25 American Home Prod 6-(fluoro and trifluoromethyl phenyl)-3 5-diamino - 1 2 4 - triazines and substituted - 6 - phenylalkyl-3,5-diamino-1 2 4-triazines
DK153787C (en) * 1979-06-01 1989-01-16 Wellcome Found METHOD OF ANALOGUE FOR THE PREPARATION OF SUBSTITUTED 3,5-DIAMINO-6-PHENYL-1,2,4-TRIAZINES AND ALFA-CYANOBENZYLIDEEN-AMINOGUANIDE COMPOUNDS FOR USE AS INTERMEDIATES
GB9203483D0 (en) * 1992-02-19 1992-04-08 Wellcome Found Anti-inflammatory compounds

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