Method for producing...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 261/04 (2006.01) C07D 275/02 (2006.01) C07B 61/00 (2006.01)

Patent

CA 2586449

The invention provides a process for producing (4,5-dihydro- isoxazol-3- yl)thiocarboxamidine salts easily and safely in a high yield which is freed from the disadvantages of the prior art. Specifically, a process for producing (4,5-dihydro- isoxazol-3-yl)thiocarboxamidine salts represented by the general formula (2): (2) [wherein R1 and R2 are each hydrogen, alkyl, or the like; R3 and R4 are each hydrogen or alkyl; or R1 and R2 or R2 and R3 together with the carbon atom(s) to which they are bonded may form cycloalkyl; and X2 is halogen or an anionic residue derived from an acid] by reacting a 3-halogeno-4,5- dihydroisoxazole represented by the general formula (1): (1) [wherein R1, R2, R3 and R4 are each as defined above; and X1 is halogeno] with thiourea in the presence of an acid.

La présente invention concerne un procédé permettant de produire aisément, de manière sûre et avec un rendement élevé des sels de (4,5-dihydroisoxazol-3-yl)thiocarboxamidine sans les inconvénients de la technique antérieure. L~invention concerne spécifiquement un procédé de production de sels de (4,5-dihydroisoxazol-3-yl)thiocarboxamidine représentés par la formule générale (2) : (2) [dans laquelle R1 et R2 sont chacun un atome d~hydrogène, un alkyle ou un groupe similaire ; R3 et R4 sont chacun un atome d~hydrogène ou un alkyle ; ou bien R1 et R2, ou R2 et R3, peuvent former un cycloalkyle avec le ou les atomes de carbone auxquels ils sont liés ; enfin, X2 est un halogène ou un reste anionique dérivé d~un acide] par réaction d~un composé 3-halogéno-4,5-dihydroisoxazole représenté par la formule générale (1) : (1) [dans laquelle R1, R2, R3 et R4 sont tels que définis précédemment et X1 est un groupe halogéno] avec de la thiourée, en présence d~un acide.

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