- MICROBIOCIDAL QUINOLINE DIHYDRO-(THIAZINE)OXAZINE DERIVATIVES
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Compounds of formula (I), wherein the subsitiuents are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
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Page/Page column 71
(2020/05/15)
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- Samarium Diiodide Catalyzed Radical Cascade Cyclizations that Construct Quaternary Stereocenters
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SmI 2 -catalyzed radical cascade cyclizations were used to generate complex carbocyclic products bearing quaternary stereocenters with high selectivity. Bicyclic scaffolds containing four contiguous stereocenters and one quaternary stereocenter
- He, Qiong,Huang, Huan-Ming,Procter, David J.
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supporting information
p. 45 - 50
(2019/12/30)
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- Asymmetric Synthesis of Cα-Substituted Prolines through Curtin–Hammett-Controlled Diastereoselective N-Alkylation
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Asymmetric synthesis of α-substituted proline derivatives has been accomplished by an efficient chirality-transfer method. High diastereoselectivity of the N-alkylation of the proline ester (C→N chirality transfer) was achieved when a 2,3-disubstituted be
- Cho, Hyunkyung,Jeon, Hongjun,Shin, Jae Eui,Lee, Seokwoo,Park, Soojun,Kim, Sanghee
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supporting information
p. 2447 - 2451
(2019/01/30)
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- Asymmetric Cα-Alkylation of Proline via Chirality Transfers of Conformationally Restricted Proline Derivative: Application to the Total Synthesis of (-)-Amathaspiramide F
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An efficient strategy for the asymmetric synthesis of Cα-tetrasubstituted proline derivatives from proline has been established. A nitrogen-fused bicyclic system was devised to control the stereodynamics of proline. Through N-quaternizations with allylic electrophiles followed by [2,3]-rearrangements, the bicyclic proline system delivered enantioenriched Cα-tetrasubstituted prolines. This strategy was applied to the concise total synthesis of (-)-amathaspiramide F.
- Cho, Hyunkyung,Shin, Jae Eui,Lee, Seokwoo,Jeon, Hongjun,Park, Soojun,Kim, Sanghee
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supporting information
p. 6121 - 6125
(2018/10/02)
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- Palladium-catalyzed oxidative arylacetoxylation of alkenes: Synthesis of indole and indoline derivatives
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A method for the oxidative arylacetoxylation of alkenes has been developed to synthesize indole and indoline derivatives from readily accessible substrates. The cinnamyl tethered anilines with picolinamide as a directing group provided 3-substituted indoles via intramolecular oxidative arylacetoxylation, and the 2-methyl substituted cinnamyl anilines furnished indoline derivatives with 3-position quaternary stereocenters in good to excellent yields via sequential intramolecular oxidative arylacetoxylation, hydrolysis and oxidation steps.
- Karnakanti, Shuklachary,Zang, Zhong-Lin,Zhao, Sheng,Shao, Pan-Lin,Hu, Ping,He, Yun
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supporting information
p. 11205 - 11208
(2017/10/17)
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- Copper(I)-Catalyzed Allylic Substitutions with a Hydride Nucleophile
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An easily accessible copper(I)/N-heterocyclic carbene (NHC) complex enables a regioselective hydride transfer to allylic bromides, an allylic reduction. The resulting aryl- and alkyl-substituted branched α-olefins, which are valuable building blocks for synthesis, are obtained in good yields and regioselectivity. A commercially available silane, (TMSO)2Si(Me)H, is employed as hydride source. This protocol offers a unified alternative to the established metal-catalyzed allylic substitutions with carbon nucleophiles, as no adaption of the catalyst to the nature of the nucleophile is required.
- Nguyen, T. N. Thanh,Thiel, Niklas O.,Pape, Felix,Teichert, Johannes F.
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supporting information
p. 2455 - 2458
(2016/06/09)
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- Discovery of Benzocycloalkane Derivatives Efficiently Blocking Bacterial Virulence for the Treatment of Methicillin-Resistant S. aureus (MRSA) Infections by Targeting Diapophytoene Desaturase (CrtN)
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Antivirulence strategies are now attracting interest for the inherent mechanism of action advantages. In our previous work, diapophytoene desaturase (CrtN) was identified to be an attractive and drugable target for fighting pigmented S. aureus infections. In this research, we developed a series of effective benzocycloalkane-derived CrtN inhibitors with submicromolar IC50. Analogue 8 blocked the pigment biosynthesis of three MRSA strains with a nanomolar IC50 value. Corresponding to its mode of action, 8 did not function as a bactericidal agent. 8 could sensitize S. aureus to immune clearance. In vivo, 8 was proven to be efficacious in an S. aureus Newman sepsis model and abscess formation model. For two typical MRSAs, USA400 MW2 and Mu50, 8 significantly decreased the staphylococcal loads in the liver and kidneys. Moreover, 8 showed minimal antifungal activity compared to that of NTF. In summary, 8 has the potential to be developed as a therapeutic drug, especially against intractable MRSA issues.
- Wang, Youxin,Di, Hongxia,Chen, Feifei,Xu, Yong,Xiao, Qiang,Wang, Xuehai,Wei, Hanwen,Lu, Yanli,Zhang, Lingling,Zhu, Jin,Lan, Lefu,Li, Jian
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p. 4831 - 4848
(2016/06/13)
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- Biphilic organophosphorus catalysis: Regioselective reductive transposition of allylic bromides via PIII/PV redox cycling
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We report that a regioselective reductive transposition of primary allylic bromides is catalyzed by a biphilic organophosphorus (phosphetane) catalyst. Spectroscopic evidence supports the formation of a pentacoordinate (σ5-P) hydridophosphorane as a key reactive intermediate. Kinetics experiments and computational modeling are consistent with a unimolecular decomposition of the σ5-P hydridophosphorane via a concerted cyclic transition structure that delivers the observed allylic transposition and completes a novel PIII/PV redox catalytic cycle. These results broaden the growing repertoire of reactions catalyzed within the PIII/PV redox couple and suggest additional opportunities for organophosphorus catalysis in a biphilic mode.
- Reichl, Kyle D.,Dunn, Nicole L.,Fastuca, Nicholas J.,Radosevich, Alexander T.
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supporting information
p. 5292 - 5295
(2015/05/13)
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- Catalytic asymmetric claisen rearrangement of enolphosphonates: Construction of vicinal tertiary and all-carbon quaternary centers
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A copper-catalyzed enantioselective Claisen rearrangement of easily accessible enolphosphonates using the commercially available PhBOX as the chiral ligand was developed. A wide range of rearrangement products with contiguous tertiary and all-carbon quaternary centers were obtained in excellent yields and stereoselectivities. The α-ketophosphonate substituent in the products could be easily transformed into other functional groups. Copyright
- Tan, Jiajing,Cheon, Cheol-Hong,Yamamoto, Hisashi
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supporting information; experimental part
p. 8264 - 8267
(2012/09/08)
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- Copper-catalyzed nucleophilic trifluoromethylation of allylic halides: A simple approach to allylic trifluoromethylation
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Trifluoromethylation: The treatment of allylic halides with trifluoromethyltrimethylsilane in the presence of a catalytic amount of copper(I) thiophene-2-carboxylate (CuTC) gives the corresponding allylic trifluoromethylation products in good to high yields and with complete regioselectivity (see scheme). The use of THF as a solvent is crucial for obtaining good yields of product.
- Miyake, Yoshihiro,Ota, Shin-Ichi,Nishibayashi, Yoshiaki
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supporting information
p. 13255 - 13258
(2012/11/07)
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- Catalytic, enantioselective intramolecular hydroamination of primary amines tethered to Di- and trisubstituted alkenes
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The in situ preparation of chiral amido alkyl ate yttrium complexes from an array of chiral N-benzyl-like-substituted binaphthyldiamines is reported. These chiral heteroleptic complexes are shown to be efficient catalysts for the enantioselective intramolecular hydroamination of primary amines tethered to sterically demanding alkenes at high reaction temperatures. Fine tuning of their chiral environment allowed up to 77% ee to be reached for the cyclization of aminoalkenes bearing 1,2-dialkyl-substituted carbon-carbon double bonds. These chiral complexes also demonstrate the ability to promote the cyclization of amine-tethered trisubstituted alkenes in up to 55% ee, as the first report of the formation of enantioenriched quaternary centers by an hydroamination reaction.
- Chapurina, Yulia,Ibrahim, Houssein,Guillot, Regis,Kolodziej, Emilie,Collin, Jacqueline,Trifonov, Alexander,Schulz, Emmanuelle,Hannedouche, Jerome
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experimental part
p. 10163 - 10172
(2012/01/15)
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- Asymmetric lithiation-substitution sequences of substituted allylamines
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(-)-Sparteine-mediated asymmetric lithiation-substitution sequences of 2- and 3-substituted N-(Boc)-N-(p-methoxyphenyl) allylic amines with electrophiles have been investigated. Asymmetric lithiation-substitutions of N-(Boc)-N-(p-methoxyphenyl) allylic am
- Kim, Dwight D.,Lee, Suk Joong,Beak, Peter
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p. 5376 - 5386
(2007/10/03)
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- Reactivity of 1-Cyclopropene-1-carboxylic Acid Lactones Dependent on the Size of the Lactone Ring
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The reaction of the bicyclic γ-lactone 1 with KOtBu leads to lactone 3 by addition of tert-butoxide at the 1-position of the intermediate cyclopropene lactone 2 and subsequent exo-protonation.In contrast, the δ-lactone 13, readily available from cinnamyl
- Frenking, Gernot,Huelskaemper, Ludwig,Weyerstahl, Peter
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p. 2826 - 2835
(2007/10/02)
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