An improved process for the preparation of telmisartan, or a pharmaceutically acceptable salt thereof, comprises subjecting 1H-Benzimidazole-2-n-propyl-4-methyl-6-(1′-methyl benzimidazole-2′yl) of formula (II), and methyl-4-(bromomethyl)biphenyl-2-carboxylate of formula (III) to condensation and hyd
An improved process for the preparation of telmisartan, or a pharmaceutically acceptable salt thereof, comprises subjecting 1H-Benzimidazole-2-n-propyl-4-methyl-6-(1′-methyl benzimidazole-2′yl) of formula (II), and methyl-4-(bromomethyl)biphenyl-2-carboxylate of formula (III) to condensation and hydrolysis in a single step:
대표청구항▼
1. A process for the preparation of telmisartan of formula (I), or a pharmaceutically acceptable salt thereof: characterised in that 1H-Benzimidazole-2-n-propyl-4-methyl-6-(1′methyl benzimidazole-2′yl) of formula (II) and methyl-4-(bromomethyl)biphenyl-2-carboxylate of formula (III) are subjected to
1. A process for the preparation of telmisartan of formula (I), or a pharmaceutically acceptable salt thereof: characterised in that 1H-Benzimidazole-2-n-propyl-4-methyl-6-(1′methyl benzimidazole-2′yl) of formula (II) and methyl-4-(bromomethyl)biphenyl-2-carboxylate of formula (III) are subjected to condensation and hydrolysis in a single step: followed by pH adjustment using an aqueous acid,wherein intermediate compounds of formulae (II) and (III) are reacted in dimethyl sulphoxide in the presence of a base,wherein further to pH adjustment telmisartan is extracted into dichloromethane and then isolated from acetone, andwhich prepares telmisartan Form A. 2. The process according to claim 1, wherein said base is an alkali metal hydroxide. 3. The process according to claim 1, which is carried out at a temperature in the range of about 10 to 80° C. 4. The process according to claim 3, which is carried out at a temperature in the range of about 25 to 50° C. 5. The process according to claim 1, wherein said pH is adjusted to be in the range of about 3 to 4.5. 6. The process according to claim 1, wherein said aqueous acid is acetic acid. 7. The process according to claim 1, wherein telmisartan is isolated as a free acid. 8. The process according to claim 7, wherein telmisartan free acid is optionally converted to a pharmaceutically acceptable salt thereof. 9. The process according to claim 8, wherein telmisartan is the sodium or potassium salt thereof. 10. The process according to claim 1, which prepares telmisartan, or a pharmaceutically acceptable salt thereof, with a purity of at least about 97%. 11. The process according to claim 1, which prepares telmisartan, or a pharmaceutically acceptable salt thereof, in a yield of about 80-88%. 12. The process according to claim 2, which is carried out at a temperature in the range of about 10 to 80° C. 13. The process according to claim 2, wherein said pH is adjusted to be in the range of about 3 to 4.5. 14. The process according to claim 12, wherein said aqueous acid is acetic acid. 15. The process according to claim 13, wherein said aqueous acid is acetic acid. 16. The process according to claim 12, which prepares telmisartan, or a pharmaceutically acceptable salt thereof, with a purity of at least about 97%. 17. The process according to claim 12, which prepares telmisartan, or a pharmaceutically acceptable salt thereof, in a yield of about 80-88%. 18. The process according to claim 13, which prepares telmisartan, or a pharmaceutically acceptable salt thereof, with a purity of at least about 97%. 19. The process according to claim 13, which prepares telmisartan, or a pharmaceutically acceptable salt thereof, in a yield of about 80-88%. 20. The process according to claim 14, which prepares telmisartan, or a pharmaceutically acceptable salt thereof, with a purity of at least about 97%. 21. The process according to claim 14, which prepares telmisartan, or a pharmaceutically acceptable salt thereof, in a yield of about 80-88%.
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이 특허에 인용된 특허 (3)
Hauel Norbert (Schemmerhofen DEX) Narr ; deceased Berthold (late of Biberach DEX by Elisabeth Narr ; legal representative ) Ries Uwe (Biberch DEX) van Meel Jacobus C. A. (Mittelbiberach DEX) Wienen W, Benzimidazoles useful as angiotensin-11 antagonists.
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