Invention Grant
US08410285B2 2′-halobiphenyl-4-yl intermediates in the synthesis of angiotensin II antagonists
失效
2'-卤代联苯-4-基中间体在合成血管紧张素II拮抗剂
- Patent Title: 2′-halobiphenyl-4-yl intermediates in the synthesis of angiotensin II antagonists
- Patent Title (中): 2'-卤代联苯-4-基中间体在合成血管紧张素II拮抗剂
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Application No.: US12933617Application Date: 2009-03-19
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Publication No.: US08410285B2Publication Date: 2013-04-02
- Inventor: Anton Copar , Zdenko Casar , Andrej Premrl
- Applicant: Anton Copar , Zdenko Casar , Andrej Premrl
- Applicant Address: SI Ljubljana
- Assignee: LEK Pharmaceuticals D.D.
- Current Assignee: LEK Pharmaceuticals D.D.
- Current Assignee Address: SI Ljubljana
- Agency: Arent Fox LLP
- Priority: EP08153084 20080320; EP08153085 20080320
- International Application: PCT/EP2009/053267 WO 20090319
- International Announcement: WO2009/115584 WO 20090924
- Main IPC: C07D235/08
- IPC: C07D235/08

Abstract:
A process for obtaining 2′-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental mental halogen. In addition, the coupling of arised 2′-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1′-methylbenzimidazole-2-il)benzimidazole to afford 3′-(2′-halo-biphenyl-4-ylmethyl)-1,7′-dimethyl-2′-propyl-1H,3′H-[2,5′]bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described. Further described is use of in line analytics for monitoring the aforementioned reactions, process for preparing a pharmaceutical composition and/or dosage for, or use in preparing a medicament.
Public/Granted literature
- US20110105539A1 2'-HALOBIPHENYL-4-YL INTERMEDIATES IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS Public/Granted day:2011-05-05
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