A convenient four-component one-pot strategy toward the synthesis of pyrazolo[3,4-d]pyrimidines

• Mingxing Liu,
• Jiarong Li,
• Hongxin Chai,
• Kai Zhang,
• Deli Yang,
• Qi Zhang and
• Daxin Shi

Beilstein J. Org. Chem. 2015, 11, 2125–2131, doi:10.3762/bjoc.11.229

• important because of their biological activity [1][2][3][4][5][6]. They have shown a wide range of pharmacological potential such as kinase inhibitors [1], antitumor [7][8], anti-inflammatory [9][10], antimicrobial [11][12][13], pesticides [14], radio protectant [15] and cardiovascular activity [16][17

Electrochemical selenium- and iodonium-initiated cyclisation of hydroxy-functionalised 1,4-dienes

• Philipp Röse,
• Steffen Emge,
• Jun-ichi Yoshida and
• Gerhard Hilt

Beilstein J. Org. Chem. 2015, 11, 174–183, doi:10.3762/bjoc.11.18

• are in turn potential substrates for the synthesis of functionalised heterocycles. Particularly, we were interested in the synthesis of tetrahydrofuran and pyran derivatives. Those heterocycles are prevalent substructures in many natural compounds, pesticides and drugs with antifungal and

Removal of volatile organic compounds using amphiphilic cyclodextrin-coated polypropylene

• Ludmilla Lumholdt,
• Sophie Fourmentin,
• Thorbjørn T. Nielsen and
• Kim L. Larsen

Beilstein J. Org. Chem. 2014, 10, 2743–2750, doi:10.3762/bjoc.10.290

• in order to improve the aquatic ecosystem [1]. Later in 2008, the EU elaborated on the Water Framework Directive defining several problematic compounds, including various pesticides, endocrine disruptors, and hydrocarbons such as benzene and benzene derivatives, as compounds requiring immediate and

Encapsulation of biocides by cyclodextrins: toward synergistic effects against pathogens

• Véronique Nardello-Rataj and
• Loïc Leclercq

Beilstein J. Org. Chem. 2014, 10, 2603–2622, doi:10.3762/bjoc.10.273

• ], chlorhexidine [27] and iodine [28]. In the case of pesticides, their impact on the environment is not harmless (e.g., some herbicides have an influence on bees) [29]. To improve their bioactivity as well as their stability on storage, their physicochemical characteristics, biocides can be easily encapsulated by

• resistant to these biocides. In contrast, nicotinoid and pyrethroid do not have any disadvantage with respect to resistance. Since encapsulation of these pesticides can be easily performed with CDs, the stability of β-CD inclusion complexes of various biocides (bendiocarb, neonicotinoid and pyrethroid

Electrocarboxylation: towards sustainable and efficient synthesis of valuable carboxylic acids

• Roman Matthessen,
• Jan Fransaer,
• Koen Binnemans and
• Dirk E. De Vos

Beilstein J. Org. Chem. 2014, 10, 2484–2500, doi:10.3762/bjoc.10.260

• from dimethyl phthalate and tert-butyltoluene, respectively (Scheme 5). After separation, by distillation and precipitation, both products can be used in the production of pesticides [34]. This is an example of a paired electrosynthesis, in which the anodic and cathodic reactions simultaneously form

Regioselective S_N2' Mitsunobu reaction of Morita–Baylis–Hillman alcohols: A facile and stereoselective synthesis of α-alkylidene-β-hydrazino acid derivatives

• Silong Xu,
• Jian Shang,
• Junjie Zhang and
• Yuhai Tang

Beilstein J. Org. Chem. 2014, 10, 990–995, doi:10.3762/bjoc.10.98

• –Hillman; SN2' reaction; Introduction Hydrazines and their derivatives are an important class of compounds in organic chemistry. They are widely used in the fields of pesticides, polymers, dyestuff, and pharmaceutical agents [1]. They are also versatile building blocks for accessing many important

Continuous flow nitration in miniaturized devices

• Amol A. Kulkarni

Beilstein J. Org. Chem. 2014, 10, 405–424, doi:10.3762/bjoc.10.38

• compounds are used in variety of basic chemicals, specialty chemicals, and knowledge chemicals. They are also employed in dyes, perfumes, pharmaceuticals, explosives [8], intermediates, colorants, and pesticides. In general, the annual demand for nitric acid grows in the range of 3 to 6%. A large proportion

Chemoenzymatic synthesis and biological evaluation of enantiomerically enriched 1-(β-hydroxypropyl)imidazolium- and triazolium-based ionic liquids

• Paweł Borowiecki,
• Małgorzata Milner-Krawczyk and
• Jan Plenkiewicz

Beilstein J. Org. Chem. 2013, 9, 516–525, doi:10.3762/bjoc.9.56

• enantiomers. These enantiomers can be used as chiral synthons for new drugs, pesticides or task-specific ionic liquids. The 1-(β-hydroxypropyl)-imidazole (±)-3a and -triazole (±)-3b used in this study were prepared as racemic mixtures according to the method described by Yus and co-workers [46] (Scheme 1

Inclusion of the insecticide fenitrothion in dimethylated-β-cyclodextrin: unusual guest disorder in the solid state and efficient retardation of the hydrolysis rate of the complexed guest in alkaline solution

• Dyanne L. Cruickshank,
• Natalia M. Rougier,
• Raquel V. Vico,
• Susan A. Bourne,
• Elba I. Buján,
• Mino R. Caira and
• Rita H. de Rossi

Beilstein J. Org. Chem. 2013, 9, 106–117, doi:10.3762/bjoc.9.14

• advantages of encapsulating agrochemicals such as pesticides (insecticides, herbicides, fungicides) in CDs may be gained [1], including, e.g., the conversion of toxic volatile liquids into solids, more localised pesticide application to improve delivery and reduce wastage, and stabilisation of the included

• , such as complex association constants, are also relevant parameters, especially in the context of CD-mediated remedial treatment of soils that are contaminated by persistent pesticides. As regards fenitrothion, a peripheral but important advantage of its inclusion in CDs is the significant reduction in

Derivatives of phenyl tribromomethyl sulfone as novel compounds with potential pesticidal activity

• Krzysztof M. Borys,
• Maciej D. Korzyński and
• Zbigniew Ochal

Beilstein J. Org. Chem. 2012, 8, 259–265, doi:10.3762/bjoc.8.27

• tribromomethyl phenyl sulfone derivatives as novel potential pesticides is reported. The title sulfone was obtained by following three different synthetic routes, starting from 4-chlorothiophenol or 4-halogenphenyl methyl sulfone. Products of its subsequent nitration were subjected to the SNAr reactions with

• . Keywords: 2-nitroaniline derivatives; phenylhydrazones; pesticides; SNAr reaction; tribromomethyl sulfone derivatives; Introduction The rapid growth of the world population results in a continous increase in the demand for food. At the same time, about 35% of the global crops around the world are being

• destroyed due to a diverse range of diseases as well as a wide variety of pests and weeds [1]. Both of these factors are nowadays the reason for the growing interest in the development of new, selective and efficient pesticides. Maintaining our investigations into the preparation of novel pesticidal agents

Efficient synthesis of 1,3-diaryl-4-halo-1H-pyrazoles from 3-arylsydnones and 2-aryl-1,1-dihalo-1-alkenes

• Yiwen Yang,
• Chunxiang Kuang,
• Hui Jin,
• Qing Yang and
• Zhongkui Zhang

Beilstein J. Org. Chem. 2011, 7, 1656–1662, doi:10.3762/bjoc.7.195

• and its derivatives are an important class of heterocyclic compounds. As medicines, many of them display anti-inflammatory [3], antimicrobial [3], antiplatelet [4], antiallergenic [5], antifungal [6], MAP Kinase inhibitor [7], and anticancer activities [8]. As pesticides, they are used as insecticides

Scalable synthesis of (1-cyclopropyl)cyclopropylamine hydrochloride

• Sergei I. Kozhushkov,
• Alexander F. Khlebnikov,
• Rafael R. Kostikov,
• Dmitrii S. Yufit and
• Armin de Meijere

Beilstein J. Org. Chem. 2011, 7, 1003–1006, doi:10.3762/bjoc.7.113

• )cyclopropylamine (4) have been found to be useful variously for the treatment of hepatitis C [3][4], as pest control agents [5], as inhibitors of methicillin-resistant Staphylococcus aureus [5], as pesticides, insecticides and acaricides [7][8][9][10][11][12][13] and more. This amine has been prepared from

Studies on Pd/NiFe₂O₄ catalyzed ligand-free Suzuki reaction in aqueous phase: synthesis of biaryls, terphenyls and polyaryls

• Sanjay R. Borhade and
• Suresh B. Waghmode

Beilstein J. Org. Chem. 2011, 7, 310–319, doi:10.3762/bjoc.7.41

• products, pharmaceutical intermediates, pesticides, advanced materials and liquid crystals [8][9][10]. These applications, in turn, have led to the production of biaryls and polyaryls on the industrial scale [11]. The Suzuki reaction is usually performed with homogeneous palladium catalysts in the presence

Green oxidations: Titanium dioxide induced tandem oxidation coupling reactions

• Vineet Jeena and
• Ross S. Robinson

Beilstein J. Org. Chem. 2009, 5, No. 24, doi:10.3762/bjoc.5.24

• absorbers in sunscreen lotions [3]. Its popularity stems from its inertness, low cost, and chemical stability under irradiation [4]. In the laboratory, its utility has been extended to the photodegradation of pesticides [5] and carcinogenic dyes [6], to sterilization against bacteria [7]. From a synthetic

Trifluoromethyl ethers – synthesis and properties of an unusual substituent

• Frédéric R. Leroux,
• Baptiste Manteau,
• Jean-Pierre Vors and
• Sergiy Pazenok

Beilstein J. Org. Chem. 2008, 4, No. 13, doi:10.3762/bjoc.4.13

• to attract attention in the field of chemistry and biochemistry [1]. Fluorine as a substituent in active ingredients plays a significant and increasingly important role. Currently about 15% of the pesticides listed in the 13th edition of the Pesticide Manual contain at least one fluorine atom. The

• biggest group of fluorinated pesticides are the compounds containing a trifluoromethyl group (mainly at aromatic rings), followed by aromatic compounds containing an isolated fluorine atom (one and more). However, according to the 12th and 13th edition of the pesticide manual only five pesticides

• programmes. OCF3-bearing pesticides. Mesomeric structures of the OCF3-group. Structures of 6 and 7. Conformational preference of the trifluoromethoxy group on aryl rings. Direction of π-polarization depending on the substituent as described by Schlosser et al. [57]. Preparation of trifluoromethyl ethers via

Synthesis of phosphorothioates using thiophosphate salts

• Babak Kaboudin and
• Fatemeh Farjadian

Beilstein J. Org. Chem. 2006, 2, No. 4, doi:10.1186/1860-5397-2-4

• derivatives are of interest as effective pesticides. [5][6][7][8] In recent years a number of phosphorothioates have been introduced as potential chemotherapeutic agent. [9][10][11][12] Despite their wide range of pharmacological activity, industrial and synthetic applications, the synthesis of