- PROCESS FOR PREPARING SULFONAMIDOBENZOFURAN DERIVATIVES
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The invention relates to a process for preparing 5-sulfonamido-benzofuran derivatives of general formula: formula (I) in which R represents an alkyl or aryl group and R1 and R2 represent hydrogen or an alkyl or aryl group. According to the invention, the compounds of formula I are prepared by coupling a benzofuran derivative of general formula II, where X represents chlorine, bromine or iodine or a sulfonate group: formula (II) with a sulfonamide derivative of formula R—SO2—NH2, in the presence of a basic agent and of a catalyst system formed from a complex between a palladium compound and a ligand.
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- METHOD FOR PREPARING 3-KETO-BENZOFURANE DERIVATIVES
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The invention relates to a method for preparing 3-keto-benzofurane derivatives of the general formula: Formula (I), where R is an alkyl or aryl group, R1 is hydrogen or an alkyl or aryl group, and R2 is a substituted alkyl or phenyl group. Said preparation method involves coupling a derivative of Formula III, where X is chlorine, bromine, or iodine or a sulfonate grouping: Formula (III) with a sulfonamide derivative of the formula R—SO2—NH2 in the presence of a basic agent and a catalytic system formed of a complex between a palladium compound and a ligand.
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- PREPARATION OF BENZOFURANS AND USE THEREOF AS SYNTHETIC INTERMEDIATES
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The present invention provides several synthetic methods for preparing N-(2-butylbenzofuran-5-yl)-N-(methylsulfonyl)methanesulfonamide, a compound of formula (3), an intermediate in the preparation of Dronedarone. The present invention further provides a process for preparing Dronedarone, comprising the steps of converting 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) to Dronedarone, wherein the 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) is prepared by the processes of the present invention.
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Page/Page column 34
(2011/09/15)
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- Synthesis and reduction of 5-halo-and 5-nitro-1-(benzofuran-3-yl)-2- phenylethanones
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Novel 1-(2-alkylbenzofuran-3-yl)-2-(4-methoxyphenyl)ethanones having a halogen or nitro group in position 5 of the benzofuran ring were synthesized starting with the corresponding 2-(2-formylphenoxy)alkanoic acids. 1-(2-Alkylbenzofuran-3-yl)-2-phenylethanols containing bromine or chlorine atom were prepared in high yields by reduction of the corresponding ethanones with lithium aluminum hydride. Selective catalytic reduction of nitro 1-(2-alkylbenzofuran-3-yl)-2-(4-methoxyphenyl)ethanones to the corresponding amino compounds under Pd/C in room temperature was achieved.
- Kwiecien,Szychowska
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p. 1002 - 1009
(2008/09/16)
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