2′-halobiphenyl-4-yl intermediates in the synthesis of angiotensin II antagonists

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United States of America Patent

PATENT NO 8410285
APP PUB NO 20110105539A1
SERIAL NO

12933617

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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.

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Patent Owner(s)

Patent OwnerAddress
LEK PHARMACEUTICALS D DSLOVENIA LJUBLJANA

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Casar, Zdenko Ljubljana, SI 17 26
Copar, Anton Ljubljana, SI 20 71
Premrl, Andrej Ljubljana, SI 3 1

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