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    • 2. 发明授权
    • Method for reductive elimination of protecting groups
    • 还原消除保护基团的方法
    • US4564471A
    • 1986-01-14
    • US188107
    • 1980-09-17
    • Katsumi SugiyamaHideo TakedaHiroko SatoYuji NonakaKiyotaka OyamaMasashige Kubo
    • Katsumi SugiyamaHideo TakedaHiroko SatoYuji NonakaKiyotaka OyamaMasashige Kubo
    • C07B31/00C07B51/00C07C67/00C07C227/00C07C227/16C07C227/18C07C227/20C07C231/00C07K1/06C07K1/12C07K5/075C07C101/02
    • C07K1/12C07K5/0613Y02P20/55
    • The invention provides a novel and efficient method for the elimination of protecting groups, e.g. benzyloxycarbonyl group, from a protected amino acid, peptide or derivative thereof having at least one functional group protected by a protecting group, e.g. a lower alkyl ester of N-benzyloxycarbonyl-.alpha.-L-aspartyl-L-phenylalanine by catalytic hydrogen reduction to produce free amino acid, peptide or derivative thereof. In contrast to the conventional procedures in which the reaction is carried out in a solvent dissolving both the starting compound and the product compound or a solvent dissolving the starting compound but not dissolving the product compound, the inventive method utilizes a binary two-phase reaction medium composed of water and an organic solvent not freely miscible with water such as toluene. The reaction takes place in the organic phase containing the starting compound dissolved and the catalyst dispersed therein whereas the reaction product which is water-soluble is smoothly and successively transferred into the aqueous phase so that advantages are obtained in the unexpectedly high yield of the product as well as in the easiness of handling the reaction mixture after completion of the reaction.
    • 本发明提供了一种用于消除保护基团的新型和有效的方法,例如, 苄氧羰基,被保护的氨基酸,具有至少一个被保护基保护的官能团的肽或衍生物。 N-苄氧羰基-α-L-天冬氨酰基-L-苯丙氨酸的低级烷基酯通过催化氢还原反应产生游离氨基酸,肽或其衍生物。 与在溶解起始化合物和产物化合物的溶剂或溶解起始化合物但不溶解产物化合物的溶剂中进行反应的常规方法相反,本发明的方法利用二元二相反应介质 由水和不能与水如甲苯自由混溶的有机溶剂组成。 反应发生在含有溶解的起始化合物和分散在其中的催化剂的有机相中,而水溶性的反应产物顺利地依次转移到水相中,从而获得了产品出乎意料的高产率的优点, 以及在反应完成后容易处理反应混合物。
    • 10. 发明授权
    • Fungicidal methods containing N-pyridylcarbamates
    • 含有N-吡啶基氨基甲酸盐的杀真菌剂
    • US4826859A
    • 1989-05-02
    • US838500
    • 1986-03-11
    • Tetsuo TakematsuYuji NonakaAkira NakanishiHideo Morinaka
    • Tetsuo TakematsuYuji NonakaAkira NakanishiHideo Morinaka
    • A01N47/20A01N47/22C07D213/75C07D213/76C07D401/12C07D405/12A01N43/30
    • C07D213/75A01N47/22C07D213/76C07D401/12C07D405/12
    • Fungicidal composition comprising a fungicidally effective amount of the N-pyridylcarbamate derivative having the formula (I) as an active ingredient: ##STR1## wherein X is 2-naphthyl, 5-indanyl, 5,6,7,8-tetrahydro-2-naphthyl, 1,4-methano-1,2,3,4-tetrahydro-6-naphthyl, 1,4-ethano-1,2,3,4,-tetrahydro-6-naphthyl, 2-quinolyl, or a phenyl group having one or two of the same or different substituents selected from the group of halogen atom, lower alkyl, lower alkenyl, lower alkoxy, lower alkenyloxy, halogenated lower alkyl, lower alkylthio, lower alkyl-sulfonyl, lower alkylamino, nitro, and methylenedioxy; Y is an oxygen atom or a sulfur atom; Z is lower alkyl group; W is pyridyl group having one or two of the same substituents selected from the group of lower alkyl, lower alkoxy, lower alkenyloxy, and lower alkylamino, and biologically inert carriers has excellent fungicidal activity against a variety of molds, and can be used to protect plants from fungal infections.
    • 杀真菌组合物,其包含杀真菌有效量的具有式(I)的N-吡啶基氨基甲酸酯衍生物作为活性成分:其中X是2-萘基,5-二氢化茚基,5,6,7,8-四氢 2-萘基,1,4-亚甲基-1,2,3,4-四氢-6-萘基,1,4-亚磺基-1,2,3,4-四氢-6-萘基,2-喹啉基, 或具有一个或两个相同或不同取代基的苯基,所述取代基选自卤素原子,低级烷基,低级烯基,低级烷氧基,低级烯氧基,卤代低级烷基,低级烷硫基,低级烷基 - 磺酰基,低级烷基氨基,硝基 和亚甲二氧基; Y是氧原子或硫原子; Z为低级烷基; W是具有一个或两个相同取代基的吡啶基,其选自低级烷基,低级烷氧基,低级烯氧基和低级烷基氨基,生物惰性载体对各种霉菌具有优异的杀真菌活性,可用于保护 植物从真菌感染。