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    • 4. 发明申请
    • N-PHENYLPHOSPHORSÄURETRIAMIDE, VERFAHREN ZU IHRER HERSTELLUNG UND DEREN VERWENDUNG ALS MITTEL ZUR REGULIERUNG BZW. HEMMUNG DER ENZYMATISCHEN HARNSTOFF-HYDROLYSE
    • N-苯基磷酸,METHOD FOR PRODUCING及其作为代理规管或 抑制酶活尿素水解
    • WO2006010389A1
    • 2006-02-02
    • PCT/EP2005/001157
    • 2005-02-04
    • SKW STICKSTOFFWERKE PIESTERITZ GMBHHUCKE, AndréNICLAS, Hans-JoachimWOZNIAK, HartmutMICHEL, Hans-JürgenSCHUSTER, Carola
    • HUCKE, AndréNICLAS, Hans-JoachimWOZNIAK, HartmutMICHEL, Hans-JürgenSCHUSTER, Carola
    • C07F9/22
    • C07F9/224C05B15/00C05G3/08Y02P60/218
    • Die Erfindung betrifft N -Phenylphosphorsäuretriamide der allgemeinen Formel (I), Verfahren zu ihrer Herstellung und deren Verwendung als Mittel zur Regulierung bzw. Hemmung der enzymatischen Harnstoff-Hydrolyse: In der Formel (I) bedeuten X = Sauerstoff oder Schwefel; R 1 , R 2 , R 3 , R 4 , R 5 = unabhängig voneinander Wasserstoff, C 1 -C 8 -Alkyl/Heteroalkyl, C 2 -C 8 -Alkenyl/Heteroalkenyl, C 2 -C 8 -Alkinyl/Heteroalkinyl, C 3 -C 8 -Cycloalkyl/Hetero­cycloalkyl, C 3 -C 8 -Cycloalkenyl/Heterocycloalkenyl, C 6 -C 10 -Aryl/C 5 -C 10 -Heteroaryl, Aralkyl, Heteroarylalkyl, Alkaryl, Alkheteroaryl, Alkoxy, Aryloxy, Hetaryloxy, Alkylthio, Arylthio, Hetarylthio, Acyl, Aroyl, Hetaroyl, Acyloxy, Aroyloxy, Hetaroyloxy, Alkoxycarbonyl, Aryloxycarbonyl, Hetaryloxycarbonyl, Alkylsulfonyl, Fluor, Chlor, Brom, lod, Cyano, Nitro, Sulfo, Carbonyl, Carboxy, Carbamoyl, Sulfamoyl, unter der Maßgabe, dass mindestens ein Rest R ungleich Wasserstoff ist, dass im Fall von R 1 , R 2 , R 4 , R 5 = H R 3 ungleich Nitro oder Cyano ist und dass im Fall von R 1 = Cl oder R 1 , R 3 = Cl mindestens einer der verbleibenden Reste ungleich Wasserstoff ist.
    • 本发明涉及通式(I),它们的制备方法以及它们作为用于调节或酶促水解尿素的抑制剂的用途的N-苯基磷酸:在式(I),X =氧或硫; [R 1 ,R 2 ,R 3 ,R 4 ,R 5 = 独立地为氢,C 1 -C 8 烷基/杂烷基,C 2 -C 8 烯/ 杂烯基,C 2 -C 8 炔基/杂炔基,C 3 -C 8 - 环烷基/杂环烷基, ç 3 -C 8 环烯基/杂环烯基,C 6 -C 10 - 芳基/ C 5 -C 10 - 杂芳基,芳烷基,杂芳基烷基,烷芳基,烷杂芳基,烷氧基,芳氧基,杂芳氧基,烷硫基,芳硫基,杂芳硫基,酰基,芳酰基,杂芳酰基,酰氧基,芳酰氧基,Hetaroyloxy, 烷氧基羰基,芳氧基羰基,Hetaryloxycarbonyl,烷基磺酰基,氟,氯,溴,碘,氰基,硝基,磺基,羰基,羧基,氨基甲酰基,氨磺酰基,条件是至少一个R不是氢,R中<的情况下SUP > 1 ,R 2 ,R 4 ,R 5 = HR 3 不等于硝基或氰基 并且,在R的情况下< SUP> 1 =氯或R 1 ,R 3 = Cl为基准的剩余基团中的至少一个不为氢。
    • 5. 发明申请
    • 1,2,4- THIADIAZOL-5-THIO COMPOUNDS AND THE DERIVATIVES THEREOF, METHODS FOR THE PRODUCTION THEREOF AND USE THEREOF AS UREASE AND NITRIFICATION INHIBITORS
    • 1,2,4-噻二唑基-5-硫代及其衍生物,METHOD FOR PRODUCING及其作为脲酶和硝化抑制剂
    • WO2005007636B1
    • 2005-04-07
    • PCT/EP2004006269
    • 2004-06-09
    • PIESTERITZ STICKSTOFFPALMER THOMASNICLAS HANS-JOACHIMSCHUSTER CAROLAMICHEL HANS-JUERGENGRABARSE MARGRITHUCKE ANDRE
    • PALMER THOMASNICLAS HANS-JOACHIMSCHUSTER CAROLAMICHEL HANS-JUERGENGRABARSE MARGRITHUCKE ANDRE
    • C07D285/08
    • C07D285/08
    • The invention relates to methods for the production and use of novel 1,2,4-thiadiazols of general formulae (I) or (II) as agents for regulating the inhibition of enzymatic urea hydrolysis, wherein R = hydrogen, C1-C8-alkyl or C6-C10-aryl and R = hydrogen, C1-C8- alkyl/heteroalkyl, C2-C8 -alkenyl/heteroalkenyl, C2-C8 -alkinyl/heteroalkinyl, C3-C8- cycloalkyl/heterocycloalkyl, C3-C8 -cycloalkenyl/heterocycloalkenyl, C6-C10 -aryl/heteroaryl, aralkyl, heteroarylalkyl, alkaryl, akheteroaryl, alkoxy, aryloxy, hetaryloxy, alkylthio, arylthio, hetarylthio, acyl, aroyl, hetaroyl, acyloxy, aroyloxy, hetaroyloxy, alkoxycarbonyl, aryloxycarbonyl, hetaryloxycarbonyl, amino, alkylamino, dialkylamino, alkylsulfonyl, arylsulfonyl, fluorine, chlorine, bromine, iodine, hydroxy, cyano, nitro, sulfo, carbonyl, carboxy, carbamoyl, sulfamoyl, the radicals R and/or R can, optionally, be per se and individually substituted by one or several of the above-mentioned groups. With a limited spectrum of substituents in R , said compounds can be claimed as nitrification inhibitors. The inventive 1,2,4-thiadiazols thus used are effective urease inhibitors and have a good resistance to hydrolysis and can be produced according to known methods. They are also effective nitrification inhibitors and can delay transformation of ammonia. They are the first inhibitors which effectively eliminate the two main sources of loss during the application of manure, i.e. urease-catalyzed urea hydrolysis and nitrification of ammonia nitrogen. The inventive compounds can also be combined with more potent nitrification inhibitors, whereby nitrogen losses can also be reduced, without any problem.
    • 存在用于生产和使用的通式(I)或(II)描述为用于调节或抑制酶水解尿素的装置,其中R <1> =氢,C 1新1,2,4-噻二唑的方法 C8-烷基或C6-C10芳基并且R <2> =氢,C1-C8烷基/杂烷基,C2-C8链烯基/杂,C2-C8炔基/杂炔基,C3-C8环烷基/杂环烷基,C3 C8环烯基/杂环烯基,C6-C10芳基/杂芳基,芳烷基,杂芳基烷基,烷芳基,烷杂芳基,烷氧基,芳氧基,杂芳氧基,烷硫基,芳硫基,杂芳硫基,酰基,芳酰基,杂芳酰基,酰氧基,芳酰氧基,Hetaroyloxy,烷氧基羰基,芳氧基羰基, Hetaryloxycarbonyl,氨基,烷基氨基,二烷基氨基,烷基磺酰基,芳基磺酰基,氟,氯,溴,碘,羟基,氰基,硝基,磺基,羰基,羧基,氨基甲酰基,是指氨磺酰基,其中基团R <1>和/或R <2 >本身任选和独立地被一个或多个上述基团的取代 可以被取代。 用中的R <2>有限Substituentenspektrum,所述化合物都声明为硝化抑制剂。 根据本发明所使用的1,2,4-噻二唑类提供具有被并且可通过已知的方法制备水解良好的电阻有效的脲酶。 他们还充当硝化抑制剂和能延缓铵转化。 因此,它们可以消除损耗的两个主要来源在施肥铵氮损失的脲酶水解尿素和硝化第一抑制剂。 本发明的化合物可以与除了有效的硝化抑制剂,由此可以实现的氮损失的额外还原可以容易地组合。