- PROCESS FOR THE PREPARATION OF PYRIDINE COMPOUNDS
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A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers, wherein Q is ═CR8— or ═N—; each R1, R2, R3, R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and —N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; and each R5, R6, R7, R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), to said compound of formula (I), in the presence of a catalyst, if necessary in an organic solvent.
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Page/Page column 4
(2008/06/13)
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- A process for the preparation of pyridine compounds
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A process for the preparation of a compound of formula (I) or a salt thereof, both as the isomeric mixture and the individual isomers, wherein Q is =CR8- or =N-; each R1, R2, R3 and R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and - N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; and each R5, R6, R7 and R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), or a salt thereof, wherein Q, R1, R2, R3, R4, R5, R6 and R7 are as defined above, to said compound of formula (I), or a salt thereof, in the presence of a catalyst, if necessary in an organic solvent; and, if desired, converting a compound of formula (I) to a salt thereof to another compound of formula (I); and/or, if desired, resolving an isomeric mixture of a compound of formula (I) in the individual isomers.
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- PROCESS FOR THE PREPARATION OF PANTOPRAZOLE
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The present invention is related to a new process for the preparation of pantoprazole (I) and pharmaceutical acceptable salts thereof, with a good yield and a high purity. In said process, the introduction of the methoxy group is carried over the position 4 of the piridine ring of compound (IV) by substitution of the chlorine atom, by the reaction with an alkaline methoxide in a mixture of methanol and an aprotic polar solvent. Also an aspect of the invention is an isolating process that includes a method for the purification of pantoprazole, and a process for the preparation of compound (IV), which is used as starting product for the preparation of pantoprazole.
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Page/Page column 11-12
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- A process for the preparation of pantoprazole and salts thereof
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A process for the preparation of pantoprazole and the salts thereof, comprising the reaction of a mercaptoimidazole with a picoline, to give a 2-pyridinyl-methylsulfinyl-2-benzimidazole intermediate, the oxidation thereof with ε-phthalimidoperhexanoic acid and the subsequent methoxylation.
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Page/Page column 5
(2010/02/11)
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- Process for the preparation of pantoprazole and salts thereof
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A process for the preparation of pantoprazole and the salts thereof, comprising the reaction of a mercaptoimidazole with a picoline, to give a 2-pyridinyl-methylsulfinyl-2-benzimidazole intermediate, the oxidation thereof with ε-phthalimidoperhexanoic acid and the subsequent methoxylation.
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Page/Page column 3
(2010/02/11)
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- Process for the preparation of organic compounds containing a sulfinyl or sulfonyl group in the presence of epsilon-phthalimidoperhexanoic acid
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A process for the oxidation of thioethers to sulfoxides or sulfones or for the oxidation of sulfoxides to sulfones by treatment of thioethers or sulfoxides with an oxidizing amount of ε-phthalimidoperhexanoic acid is particularly useful for the preparation of compounds of industrial interest, in particular pharmaceuticals for human or veterinary use.
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- Process for the preparation of organic compounds containing a sulfinyl or sulfonyl group
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A process for the oxidation of thioethers to sulfoxides or sulfones or for the oxidation of sulfoxides to sulfones by treatment of thioethers or sulfoxides with an oxidizing amount of ε-phthalimidoperhexanoic acid is particularly useful for the preparation of compounds of industrial interest, in particular pharmaceuticals for human or veterinary use.
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