Process for the preparation of 2,3-dihydrothiepine derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 337/08 (2006.01) C07C 323/22 (2006.01) C07C 323/52 (2006.01) C07D 337/04 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2373464

A process for preparing simply and inexpensively 2,3-dihydrothiepine derivatives represented by general formula (I) [wherein R1 is an electron- attracting group; R2, R3, R4, R5, R6 and R7 are each hydrogen, halogeno, optionally substituted amino, optionally substituted hydroxyl, an optionally substituted thiol group, optionally substituted hydrocarbyl, or an optionally substituted heterocyclic group, or R6 and R7 may be united to form a ring; and R8 is hydrogen or optionally substituted hydrocarbyl] or salts thereof, characterized by subjecting a compound represented by general formula (II) [wherein each symbol is as defined above] or a salt thereof to ring-closing reaction.

L'invention concerne un procédé permettant de préparer de manière simple et peu coûteuse des dérivés de 2,3 dihydrothiépine représentés par la formule générale (I). R?1¿ est un groupe attirant des électrons; R?2¿, R?3¿, R?4¿, R?5¿, R?6¿ et R?7¿ représentent chacun hydrogène, halogéno, amino éventuellement substitué, hydroxyle éventuellement substitué, un groupe thiol éventuellement substitué, hydrocarbyle éventuellement substitué, ou un groupe hétérocyclique éventuellement substitué, R?6¿ et R?7¿ pouvant être unis pour former un noyau; et R?8¿ représente hydrogène ou un hydrocarbyle éventuellement substitué; ou leurs sels. Le procédé consiste à soumettre un composé représenté par la formule (II), dans laquelle chaque symbole est défini comme ci-dessus, ou un sel de celui-ci, à une réaction de fermeture de noyau.

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