Sanofi

Philippe Vayron

Xavier Bon

Julia Mateos-Caro

Thomas Priem

Corinne Leroy

Bernard Grimaud

Frederic Bailly

Denis Largeau

Sylvie Vigne

Christine Biencourt

Fréderic Bailly

Frédéric Bailly

Irina Malejonock

Jean-Louis Delepine

Laure Jourdin

Vincent Ferey

Régis Mondiere

Regis Mondiere

The invention relates to a method for preparing 5-amino-benzoyl-benzofuran derivatives having the general formula in which Ris hydrogen or an alkyl or aryl group and Ris hydrogen, an alkyl, alkoxy or dialkylaminoalkoxy group. According to the invention, the compounds having formula I are prepared by hydrogenating a 5-nitro-benzofuran derivative having the general formula in which Rand Rhave the same meaning as above in the presence of palladized charcoal as a catalyst and in an ether or a mixture of ether as a solvent, thus forming the desired compounds.

Method for preparing 5-amino-benzoyl-benzofuran derivatives

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 Rand Rrepresent 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&#x2014;SO&#x2014;NH, in the presence of a basic agent and of a catalyst system formed from a complex between a palladium compound and a ligand. 

Process for preparing sulfonamidobenzofuran derivatives

The disclosure relates to a process for preparing 5-aminobenzoylbenzofuran derivatives of formula I: in which Rand Rare as defined in the disclosure; by reduction of a 5-nitrobenzofuran derivative of formula II: using a hydrogen transfer agent, in the presence of palladium-on-charcoal as catalyst and in an ether or an ether mixture as solvent.

Process for preparing aminobenzoylbenzofuran derivatives

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, Ris hydrogen or an alkyl or aryl group, and Ris 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&#x2014;SO&#x2014;NHin the presence of a basic agent and a catalytic system formed of a complex between a palladium compound and a ligand.

Method for preparing 3-keto-benzofurane derivatives

The present disclosure relates to ketobenzofuran derivatives of the general formula (I): as well as to a method of synthesizing the same by coupling a quinonimine and an enaminone by a Nenitzescu reaction and to the intermediates of the synthesis thereof.

Ketobenzofuran derivatives, method for synthesizing same, and intermediates

The disclosure relates to a process for preparing benzofuran derivatives of general formula I: in which R, R, and Rare as defined in the disclosure; by coupling the hydroxylamine with a diketone of general formula III: in order to form an oxime that is then cyclized by heating in order to form the desired compound.

Process for preparing benzofuran derivatives substituted at position 5

The invention relates to a method of synthesis of ferroquine of formula (F) or of its metabolite of formula (Fm):  

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Paris, France

Philippe Vayron