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1. 发明申请

WO2005105774A1 PROCESS FOR THE PREPARATION OF 3-(3,4-METHYLENEDIOXYPHENYL)-2-METHYLPROPANAL 审中-公开
标题翻译：制备3-（3,4-亚甲基二苯基）-2-甲基丙酸的方法
公开(公告)号：WO2005105774A1
公开(公告)日：2005-11-10
申请号：PCT/EP2005/051953
申请日：2005-04-29
申请人： ENDURA S.P.A. , BORZATTA, Valerio , CAPPARELLA, Elisa , POLUZZI, Elisa
发明人： BORZATTA, Valerio , CAPPARELLA, Elisa , POLUZZI, Elisa
IPC分类号： C07D317/26
CPC分类号： C07D317/26
摘要： Process for the preparation of 3-(3,4-methylenedioxyphenyl)-2-methylpropanal (I) comprising the following steps: a) reacting 5-propanoyl-1,3- benzodioxol (III) with the Vilsmeier reagent at temperatures ranging between 0° and 40°C and subsequently treating of the reaction mixture with a base in aprotic apolar solvent to obtain the unsaturated chloroaldehyde of formula (IV); b) reacting the unsaturated chloroaldehyde of formula (IV), obtained in the previous step, with hydrogen in the presence of a supported heterogeneous catalyst containing a metal chosen amongst Pd, Pt, Rh, Ru in the presence of an organic base or of a mixture of an organic and inorganic base.
摘要翻译：制备3-（3,4-亚甲二氧基苯基）-2-甲基丙醛（I）的方法，包括以下步骤：a）将5-丙酰基-1,3-苯并间二氧杂环戊烯（III）与Vilsmeier试剂反应，温度范围为0 °和40℃，随后用非质子非极性溶剂中的碱处理反应混合物，得到式（IV）的不饱和氯醛; b）使在前一步骤中获得的式（IV）的不饱和氯醛与氢气在有机碱存在下，在含有选自Pd，Pt，Rh，Ru中的金属的负载型非均相催化剂存在下反应，有机和无机碱的混合物。

2. 发明申请

WO2012123714A1 COMPOSITIONS AND METHODS FOR CONTROLLING PESTICIDE RESISTANT PESTS 审中-公开
标题翻译：用于控制杀虫剂抗菌剂的组合物和方法
公开(公告)号：WO2012123714A1
公开(公告)日：2012-09-20
申请号：PCT/GB2012/050500
申请日：2012-03-07
申请人： ROTHAMSTED RESEARCH LIMITED , ENDURA S.P.A. , MOORES, Graham David , PHILIPPOU, Despina , BORZATTA, Valerio , CAPPARELLA, Elisa
发明人： MOORES, Graham David , PHILIPPOU, Despina , BORZATTA, Valerio , CAPPARELLA, Elisa
IPC分类号： A01N25/22 , A01N43/40 , A01N47/40 , A01N51/00 , A01P7/00
CPC分类号： A01N43/50 , A01N43/30 , A01N51/00 , A01N43/40 , A01N47/40 , A01N2300/00 , A01N31/04 , A01N31/16 , A01N43/12
摘要： Provided are compositions comprising (i) a neonicotinoid; and (ii) a compound of formula (I) or (II), preferably wherein the composition is a pesticide composition, for example an insecticide composition. Also provided is use of a compound of formula (I) or (II) as a neonicotinoid synergist and use of a compound of formula (I) or (II) in combination with a neonicotinoid. Further provided are methods for controlling pests.
摘要翻译：提供的组合物包含（i）新烟碱类; 和（ii）式（I）或（II）的化合物，优选其中组合物是农药组合物，例如杀虫剂组合物。还提供了式（I）或（II）化合物作为新烟碱类增效剂的用途，以及式（I）或（II）化合物与新烟碱类的组合的用途。还提供了防治害虫的方法。

3. 发明申请

WO2005042512A1 PROCESS FOR SYNTHESISING HELIOTROPINE AND ITS DERIVATIVES 审中-公开
标题翻译：合成有机化合物及其衍生物的方法
公开(公告)号：WO2005042512A1
公开(公告)日：2005-05-12
申请号：PCT/EP2004/052710
申请日：2004-10-28
申请人： ENDURA S.P.A. , BORZATTA, Valerio , CAPPARELLA, Elisa , GOBBI, Carlotta , POLUZZI, Elisa
发明人： BORZATTA, Valerio , CAPPARELLA, Elisa , GOBBI, Carlotta , POLUZZI, Elisa
IPC分类号： C07D317/54
CPC分类号： C07D317/54
摘要： A new high-yield, easily industrialized process for synthesising compounds of formula (IV), in which X 1 and X 2 , the same or different, are linear or branched C1-C8 alkyls, n and m are 0,1 or 2, with the proviso that n and m are not simultaneously 0; or (OX 1 )n and (OX 2 )m taken together form an O-T-O group where T is chosen from -CH 2 -, -CH 2 CH 2 , -CH 2 CH 2 CH 2 -, -C(CH 3 ) 2 -. The process comprises treating a chloromethyl derivative (I) with an alkaline acetate to form the intermediate acetylderivative (II); the intermediate (II) is to hydrolysed to form the alcohol (III); the alcohol (III) is then oxidised in the presence of air and catalysts to obtain the desired derivative (IV). The process runs its course within a short period of time, with high yields and high selectivity; in addition, the process does not require purification and separation of the intermediates and can therefore be favourably conducted in a single batch.
摘要翻译：合成式（IV）化合物的新的高产率，易于工业化的方法，其中X1和X2相同或不同，为直链或支链C1-C8烷基，n和m为0,1或2，其中条件是n和m不同时为0; 或（OX 1）n和（OX 2）m一起形成O-T-O基团，其中T选自-CH 2 - ， - CH 2 CH 2，-CH 2 CH 2 CH 2 - ， - C（CH 3）2 - 。该方法包括用碱性乙酸盐处理氯甲基衍生物（I）以形成中间体乙酰衍生物（II）; 中间体（II）被水解形成醇（III）; 然后在空气和催化剂的存在下将醇（III）氧化以获得所需的衍生物（IV）。该过程在短时间内运行，产量高，选择性高; 此外，该方法不需要中间体的纯化和分离，因此可以在单次批次中有利地进行。

4. 发明申请

WO2007012641A1 PROCESS FOR PREPARING 3,4-DIOXO-SUBSTITUTED AROMATIC ALDEHYDES 审中-公开
标题翻译：制备3,4-二氧基取代的芳族醛的方法
公开(公告)号：WO2007012641A1
公开(公告)日：2007-02-01
申请号：PCT/EP2006/064622
申请日：2006-07-25
申请人： ENDURA S.P.A. , CAPPARELLA, Elisa , POLUZZI, Elisa , BORZATTA, Valerio
发明人： CAPPARELLA, Elisa , POLUZZI, Elisa , BORZATTA, Valerio
IPC分类号： C07C45/29 , C07C47/575 , C07D317/54 , C07C47/54
CPC分类号： C07C45/29 , C07C45/68 , C07D317/54 , C07C47/575
摘要： A new process for synthesising 3,4-dioxo-substituted aromatic aldehydes by Oppenauer oxidation of the corresponding benzyl alcohols is described. The process, which specifically uses formaldehyde as hydrogen acceptor, proceeds with unexpectedly high yields and conversion percentages, allowing low cost access to finished and intermediate products of high industrial interest in the field of pharmaceutical products and fragrances.
摘要翻译：描述了通过相应的苄醇的Oppenauer氧化合成3,4-二氧代取代的芳族醛的新方法。特别使用甲醛作为氢受体的方法，出乎意料地高产率和转化率，允许低成本进入医药产品和香料领域具有高工业意义的成品和中间产品。

5. 发明申请

WO2006111570A2 NEW BIOLOGICALLY ACTIVE FORMULATION 审中-公开
标题翻译：新生物活性配方
公开(公告)号：WO2006111570A2
公开(公告)日：2006-10-26
申请号：PCT/EP2006/061724
申请日：2006-04-21
申请人： ENDURA S.P.A. , PICCOLO, Oreste , BORZATTA, Valerio , DELOGU, Giovanna , CAPPARELLA, Elisa , DE CANDIA, Cristina , GOBBI, Carlotta , DI BLASI, Giovanna
发明人： PICCOLO, Oreste , BORZATTA, Valerio , DELOGU, Giovanna , CAPPARELLA, Elisa , DE CANDIA, Cristina , GOBBI, Carlotta , DI BLASI, Giovanna
IPC分类号： A01N25/10 , A01N57/16 , A01N47/40 , A01N47/18 , A01N47/02 , A01N43/78 , A01N43/54 , A01N43/50 , A01P7/04 , A01N43/30
CPC分类号： A01N25/10
摘要： The present invention provides a formulation characterised by the simultaneous presence in cyclodextrin based supramolecular complexes, of two components, one of which possesses insecticidal, acaricidal, fungicidal, snailcidal or vermicidal activity and the other possesses an activity synergistic with the first, enhancing its effectiveness. The biologically active substance is chosen from the following classes of chemical products: carbamates, organophosphates, thioureas, pentatomic or hexatomic heterocycles in which 1 , 2 or 3 nitrogen atoms are present. The synergistic substance can be chosen from components containing at least one aromatic or non aromatic carbocyclic ring, such as piperonyl butoxide, sesamol, verbutin or MGK 264. For the same dose, the activity of the present formulations is greater than that of the mixture of the two active components alone or separately complexed with cyclodextrin. The process for preparing said formulation and its use for the activities herein indicated are further aspects of the present invention.
摘要翻译：本发明提供一种制剂，其特征在于同时存在两种组分的两种组分的基于环糊精的超分子复合物，其中一种具有杀虫，杀螨，杀真菌，杀虫或杀虫活性，另一种具有与第一种协同作用的活性，提高其有效性。生物活性物质选自以下类别的化学产品：其中存在1,2或3个氮原子的氨基甲酸酯，有机磷酸酯，硫脲，五原子或六原子杂环。协同物质可以选自含有至少一个芳族或非芳族碳环的组分，例如胡椒基丁醚，芝麻酚，鸟嘌呤或MGK 264.对于相同的剂量，本发明制剂的活性大于两种活性组分单独或分别与环糊精复合。制备所述制剂的方法及其用于本文所述活性的用途是本发明的另外的方面。

6. 发明申请

WO2006087357A3 PROCESS FOR OBTAINING ENANTIOMERS OF CHRYSANTHEMIC ACID 审中-公开
标题翻译：获得CHRYSYSTHTHIC酸的对映体的方法
公开(公告)号：WO2006087357A3
公开(公告)日：2006-09-28
申请号：PCT/EP2006060013
申请日：2006-02-16
申请人： ENDURA SPA , BORZATTA VALERIO , ROSINI GOFFREDO , AYOUB CLAUDIA , RIGHI PAOLO , CAPPARELLA ELISA
发明人： BORZATTA VALERIO , ROSINI GOFFREDO , AYOUB CLAUDIA , RIGHI PAOLO , CAPPARELLA ELISA
IPC分类号： C07C61/37 , C07C51/487 , C07C323/32
CPC分类号： C07C323/32 , C07C51/487 , C07C61/37
摘要： A new process is described, easy to perform on industrial scale, with high yield, for obtaining enantiomers of chrysanthemic acid starting from mixtures containing them. The process involves reacting said mixtures with enantiomers of 2- dimethylamino-1-phenyl-1 ,3-propanediol (DMPP) and 2-dimethylamino-1-[4- (methylthio)phenyl]propane-1 ,3-diol (MTDP) as chiral selectors. The invention includes salts of chrysanthemic acid with the aforesaid chiral selectors as process intermediates. The process allows operation in a single solvent rather than in solvent mixtures difficult to recover and reuse, and the final crystallization product does not incorporate molecules of solvent. The bases used are then recovered and reused in subsequent separations.
摘要翻译：描述了一种新的方法，易于在工业规模上进行，产率高，用于从含有它们的混合物开始获得菊酸的对映异构体。该方法包括使所述混合物与2-二甲基氨基-1-苯基-1,3-丙二醇（DMPP）和2-二甲基氨基-1- [4-（甲硫基）苯基]丙烷-1,3-二醇（MTDP）的对映异构体反应，作为手性选择器。本发明包括菊酸盐与上述手性选择剂作为工艺中间体。该方法允许在单一溶剂中操作而不是在溶剂混合物中难以回收和再利用，并且最终结晶产物不掺入溶剂分子。然后回收所用的碱，并在随后的分离中重新使用。

7. 发明申请

WO2011020848A1 SUBSTITUTED ALKYNYL PHENOXY COMPOUNDS AS NEW SYNERGISTS IN PESTICIDAL COMPOSITIONS 审中-公开
标题翻译：作为农药组合物中新的合成物的取代的烷基苯氧基化合物
公开(公告)号：WO2011020848A1
公开(公告)日：2011-02-24
申请号：PCT/EP2010/062019
申请日：2010-08-18
申请人： ENDURA S.P.A. , ROTHAMSTED RESEARCH LTD. , BORZATTA, Valerio , CAPPARELLA, Elisa , MORONI, Leni , MOORES, Graham , PHILIPPOU, Despina
发明人： BORZATTA, Valerio , CAPPARELLA, Elisa , MORONI, Leni , MOORES, Graham , PHILIPPOU, Despina
IPC分类号： A01N43/08 , A01N43/30
CPC分类号： C07C41/16 , A01N43/30 , C07C43/215 , A01N51/00 , A01N53/00
摘要： A composition comprising an alkynyl phenoxy compound of Formula (I) as a synergist and a pesticidal active ingredient is described, wherein R 1 and R 2 , similar or different, are (C 1 -C 4 )alkyl or R 1 O- and R 2 O- together represent a group -O-CH 2 -O-, -O- CH(CH 3 )-O, -O-CH 2 -CH 2 -O-, -O-CH 2 -CH 2 -, R 3 is (C 1 -C 6 )alkyl, (C 3 -C 6 )alkenyl or -B- (CH 2 -CH 2 -O)z-R 6 where B is -CH 2 -O- or -O-, z is 0, 1 or 2 and R 6 is (C 1 -C 4 )alkyl;R 4 is hydrogen or methyl;R 5 is hydrogen or methyl;x is an integer from 1 to 2; y is 0, 1 or 2; with the proviso that when R 3 is -B-(CH 2 -CH 2 -O)z-R 6 , y is 1 and 5-(propargyloxy)- benzo[1,3]dioxole is excluded.
摘要翻译：描述了包含作为增效剂的式（I）炔基苯氧基化合物和杀虫活性成分的组合物，其中相同或不同的是（C1-C4）烷基或R1O-和R2O-一起代表基团 - O-CH 2 -O - ， - CH（CH 3）-O，-O-CH 2 -CH 2 -O - ， - O-CH 2 -CH 2 - ，R 3是（C 1 -C 6）烷基，（C 3 -C 6）或-B-（CH 2 -CH 2 -O）z -R 6，其中B是-CH 2 -O-或-O-，z是0,1或2，R 6是（C 1 -C 4）烷基; R 4是氢或甲基; R5是氢或甲基; x是1至2的整数; y为0,1或2; 条件是当R3为-B-（CH2-CH2-O）z-R6时，y为1，排除5-（炔丙基氧基） - 苯并[1,3]间二氧杂环戊烯。

8. 发明申请

WO2006087357A2 PROCESS FOR OBTAINING ENANTIOMERS OF CHRYSANTHEMIC ACID 审中-公开
标题翻译：获得食盐酸成分的方法
公开(公告)号：WO2006087357A2
公开(公告)日：2006-08-24
申请号：PCT/EP2006/060013
申请日：2006-02-16
申请人： ENDURA S.P.A. , BORZATTA, Valerio , ROSINI, Goffredo , AYOUB, Claudia , RIGHI, Paolo , CAPPARELLA, Elisa
发明人： BORZATTA, Valerio , ROSINI, Goffredo , AYOUB, Claudia , RIGHI, Paolo , CAPPARELLA, Elisa
IPC分类号： C07C61/37 , C07C51/487 , C07C323/32
CPC分类号： C07C323/32 , C07C51/487 , C07C61/37
摘要： A new process is described, easy to perform on industrial scale, with high yield, for obtaining enantiomers of chrysanthemic acid starting from mixtures containing them. The process involves reacting said mixtures with enantiomers of 2- dimethylamino-1-phenyl-1 ,3-propanediol (DMPP) and 2-dimethylamino-1-[4- (methylthio)phenyl]propane-1 ,3-diol (MTDP) as chiral selectors. The invention includes salts of chrysanthemic acid with the aforesaid chiral selectors as process intermediates. The process allows operation in a single solvent rather than in solvent mixtures difficult to recover and reuse, and the final crystallization product does not incorporate molecules of solvent. The bases used are then recovered and reused in subsequent separations.
摘要翻译：描述了一种新的方法，以工业规模容易地以高产率进行，以从含有它们的混合物开始获得菊酸的对映异构体。该方法包括使所述混合物与2-二甲基氨基-1-苯基-1,3-丙二醇（DMPP）和2-二甲基氨基-1- [4-（甲硫基）苯基]丙烷-1,3-二醇（MTDP）的对映异构体反应，作为手性选择器。本发明包括菊酸与上述手性选择剂的盐作为加工中间体。该方法允许在单一溶剂中操作，而不是难于回收和再利用的溶剂混合物中，并且最终结晶产物不掺入溶剂分子。然后使用的碱被回收并在随后的分离中重新使用。

9. 发明申请

WO2004092106A3 PROCESS FOR PREPARING ALKOXY- AND ARYLOXY-PHENOLS 审中-公开
标题翻译：制备烷氧基 - 和芳氧基 - 酚的方法
公开(公告)号：WO2004092106A3
公开(公告)日：2004-12-09
申请号：PCT/EP2004050470
申请日：2004-04-07
申请人： ENDURA SPA , BORZATTA VALERIO , PICCOLO ORESTE , CAPPARELLA ELISA , POLUZZI ELISA
发明人： BORZATTA VALERIO , PICCOLO ORESTE , CAPPARELLA ELISA , POLUZZI ELISA
IPC分类号： C07C41/26 , C07C43/23 , C07C67/42 , C07D317/64 , C07D319/18 , C07C43/295 , C07C69/017
CPC分类号： C07D317/64 , C07C41/26 , C07C67/42 , C07D319/18 , C07C69/017 , C07C43/295 , C07C43/23
摘要： Process for preparing alkoxy- and aryloxy-phenols, comprising oxidizing the ketone of formula (I) with peracids to give the corresponding ester of formula (II) which is then hydrolysed to give the corresponding aryloxy- or alkoxy-phenol.
摘要翻译：包括用过酸氧化式（I）的酮以得到相应的式（II）的酯，然后将其水解以得到相应的芳氧基 - 或烷氧基 - 苯酚，制备烷氧基 - 和芳氧基 - 酚。

10. 发明申请

WO2010131274A1 PROCESS FOR PREPARING HYDROCINNAMIC ALDEHYDES IN ENANTIOPURE OR ENANTIOMERICALLY ENRICHED FORM 审中-公开
标题翻译：制备放射性或充分形成的水解氢氧化物的方法
公开(公告)号：WO2010131274A1
公开(公告)日：2010-11-18
申请号：PCT/IT2009/000212
申请日：2009-05-14
申请人： ENDURA S.P.A , CAPPARELLA, Elisa , CARLONI, Silvia
发明人： CAPPARELLA, Elisa , CARLONI, Silvia
IPC分类号： C07C41/56 , C07C209/88 , C07C211/27 , C07D317/54 , C07D317/58 , C07D317/60
CPC分类号： C07D317/60 , C07B2200/07 , C07C29/147 , C07C41/56 , C07C41/58 , C07C51/285 , C07C51/487 , C07C57/30 , C07C211/27 , C07D317/54 , C07D317/58 , C07C33/20 , C07C43/303
摘要： A process is described for preparing hydrocinnamic aldehydes in enantiopure or enantiomerically enriched form of Formula I, in which R is isopropyl or tert-butyl and R' is hydrogen, or R and R' when taken together are a methylenedioxolyl group, comprising the following steps: a) reacting the hydrocinnamic aldehyde of Formula I with the alcohol of Formula Il in enantiopure or enantiomerically enriched form to give the crystallized hemiacetal of Formula III, in which R, R' have the same meaning as Formula I and (*) indicates a stereogenic centre in the absence of a solvent or in one or more aprotic solvents or mixtures thereof with apolar solvents; b) recovering the hydrocinnamic aldehyde of Formula I in enantiopure or enantiomerically enriched form from the crystallized hemiacetal of Formula III and the aldehyde of opposite configuration in enantiopure or enantiomerically enriched form from the hemiacetal crystallization mother liquors. The invention also concerns a process for preparing the alcohol of Formula Il to be introduced into step a).
摘要翻译：描述了制备式I的对映体纯或富含对映异构体形式的氢化肉桂醛的方法，其中R是异丙基或叔丁基，R'是氢，或R和R'一起是亚甲二氧基苯基，包括以下步骤：a）使式I的氢化肉桂醛与对映异构体富含形式的式II的醇反应，得到式III的结晶半缩醛，其中R，R'具有与式I相同的含义，（*）表示在不存在溶剂的情况下或在一种或多种非质子溶剂或其与非极性溶剂的混合物中的立体中心; b）从半缩醛结晶母液的结晶半缩醛和对映异构体富含形式的相反构型的醛回收具有对映异构体或对映体富集形式的式I的氢化肉桂醛。本发明还涉及制备待引入到步骤a）中的式II的醇的方法。

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