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    • 4. 发明授权
    • Process for preparing N-sulphonyl-ureas
    • 制备N-磺酰脲的方法
    • US4954628A
    • 1990-09-04
    • US317769
    • 1989-03-02
    • Gabor BesenyeiSandor NemethLaszlo SimandiMaria BelakMaria SzaboJozsef DukaiLajos NagyElemer TomordiCsaba SopteiErzsebet E. Dioszegine
    • Gabor BesenyeiSandor NemethLaszlo SimandiMaria BelakMaria SzaboJozsef DukaiLajos NagyElemer TomordiCsaba SopteiErzsebet E. Dioszegine
    • C07D251/16B01J27/13B01J31/16C07B61/00C07C311/60C07D213/75C07D239/42C07D251/18C07D251/22C07D251/46C07D333/34C07D521/00
    • C07D521/00C07C311/60
    • The invention relates to a process for preparing sulphonyl-ureas of the general formula (I) ##STR1## wherein Ar.sub.1 represents a phenyl, naphthyl or thienyl group, the derivatives thereof substituted by C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, (halo)alkoxycarbonyl, (halo)alkyloxy, nitro, cyano groups as well as by halogen atoms,Ar.sub.2 represents a phenyl, pyridyl, pirimidinyl or triazinyl group and the derivatives thereof substituted by C.sub.1-4 (halo)alkyl, C.sub.1-4 (halo)alkyloxy, amino, O-acyl, O-arylsulphonyl, O-(substituted carbamoyl) groups as well as by halogen atoms.According to the invention N-halogen aryl sulphonamidate is reacted in the presence of a carbonylating catalyst, carbon monoxide and an aromatic amine, optionally in the presence of a phase transfer catalyst, or N-halogen aryl sulphonamidate is reacted with carbon monoxide in the presence of a carbonylating catalyst, and optionally in the presence of a phase transfer catalyst, then the obtained reaction mixture is further reacted with an aromatic amine or an N-halogen-arylamine-alkali metal salt is reacted with aryl-sulphonamid in the presence of a carbonylating catalyst, carbon monoxide and optionally in the presence of a phase transfer catalyst or an amine, amine dihalogenid, aryl sulphonamid are reacted in the presence of a carbonylating catalyst and carbon monoxide and the obtained reaction mixture is worked up in a known manner.The thus prepared sulphonyl-ureas are biologically active compounds, which are used in the pharmaceutical industry and for regulating plant growth.
    • 本发明涉及一种制备通式(I)的磺酰脲的方法,其中Ar 1表示苯基,萘基或噻吩基,其衍生物被C 1-4烷基,C 1-4卤代烷基, (卤代)烷氧基羰基,(卤代)烷氧基,硝基,氰基以及卤素原子,Ar 2表示苯基,吡啶基,吡啶基或三嗪基,其衍生物被C 1-4(卤代)烷基, 卤代)烷氧基,氨基,O-酰基,O-芳基磺酰基,O-(取代的氨基甲酰基)基团以及卤素原子。 根据本发明,N-卤素芳基磺酰胺酸酯在羰基化催化剂,一氧化碳和芳族胺的存在下,任选地在相转移催化剂存在下反应,或N-卤素芳基磺酰胺盐与一氧化碳在存在下反应 的羰基化催化剂,并且任选地在相转移催化剂存在下,然后将所得反应混合物进一步与芳族胺反应或N-卤素 - 芳基胺 - 碱金属盐在芳基 - 磺酰胺存在下与 羰基化催化剂,一氧化碳和任选在相转移催化剂或胺,胺二卤代芳基磺酰胺存在下,在羰基化催化剂和一氧化碳的存在下反应,并将所得反应混合物以已知方式处理。 如此制备的磺酰脲是生物活性化合物,其用于制药工业和调节植物生长。