Bioinformatic prediction of the stereoselectivity of modular polyketide synthase: an update of the sequence motifs in ketoreductase domain

• Changjun Xiang,
• Shunyu Yao,
• Ruoyu Wang and
• Lihan Zhang

Beilstein J. Org. Chem. 2024, 20, 1476–1485, doi:10.3762/bjoc.20.131

• ), epothilone (anticancer), ivermectin (antiparasitic), and spinosyn (insecticide) [1][2]. Modular PKSs consist of multiple modules that catalyze one round of chain extension by domains with different functions and are divided into cis-acyltransferase (cis-AT) and trans-AT PKSs depending on whether AT domain is

Cyanothioacetamides as a synthetic platform for the synthesis of aminopyrazole derivatives

• Valeriy O. Filimonov,
• Alexandra I. Topchiy,
• Vladimir G. Ilkin,
• Tetyana V. Beryozkina and
• Vasiliy A. Bakulev

Beilstein J. Org. Chem. 2023, 19, 1191–1197, doi:10.3762/bjoc.19.87

• molecules that attack and destroy lipids and protein membranes of weed cells [10]. Fipronil is an inhibitor of GABA receptors and affects the nervous system of insects as a broad-spectrum insecticide [11][12]. On the other hand, thioamides are an important class of organic compounds. 6-Thioguanine and

Electrogenerated base-promoted cyclopropanation using alkyl 2-chloroacetates

• Kouichi Matsumoto,
• Yuta Hayashi,
• Kengo Hamasaki,
• Mizuki Matsuse,
• Hiyono Suzuki,
• Keiji Nishiwaki and
• Norihito Kawashita

Beilstein J. Org. Chem. 2022, 18, 1116–1122, doi:10.3762/bjoc.18.114

• recognized as important molecules. For example, cyclopropane derivatives are found in both natural products and pharmaceutical products. The cyclopropane skeleton is also found in agrochemicals, especially pyrethroid, as an insecticide, is one important compound. Cyclopropanes also play a significant role in

N-tert-Butanesulfinyl imines in the asymmetric synthesis of nitrogen-containing heterocycles

• Joseane A. Mendes,
• Paulo R. R. Costa,
• Miguel Yus,
• Francisco Foubelo and
• Camilla D. Buarque

Beilstein J. Org. Chem. 2021, 17, 1096–1140, doi:10.3762/bjoc.17.86

• piperidine alkaloids isolated from fire ants (Solenopsis) and display hemolytic, insecticide and antibiotic properties. A straightforward synthesis of these natural products from a common imine intermediate was reported by Medjahdi et

Anthelmintic drug discovery: target identification, screening methods and the role of open science

• Frederick A. Partridge,
• Ruth Forman,
• Carole J. R. Bataille,
• Graham M. Wynne,
• Marina Nick,
• Angela J. Russell,
• Kathryn J. Else and
• David B. Sattelle

Beilstein J. Org. Chem. 2020, 16, 1203–1224, doi:10.3762/bjoc.16.105

• the Medicines for Malaria Venture Pathogen Box, have been successful at facilitating screening in diverse assays against many different parasite pathogens and models. Of the compounds identified so far in these screens, tolfenpyrad, a repurposed insecticide, shows significant promise and there has

• . mansoni [161]) and the cestode E. multilocularis [162]. Perhaps the most promising lead from the Pathogen Box so far is tolfenpyrad, a pyrazole-5-carboxamide insecticide, which was first identified as an anthelmintic with activity against exsheathed L3 and L4 parasitic life stages of Haemonchus contortus

Fluorine-containing substituents: metabolism of the α,α-difluoroethyl thioether motif

• Andrea Rodil,
• Alexandra M. Z. Slawin,
• Nawaf Al-Maharik,
• Ren Tomita and
• David O’Hagan

Beilstein J. Org. Chem. 2019, 15, 1441–1447, doi:10.3762/bjoc.15.144

• compounds that are of commercial significance [8][9][10]. Metabolism studies in both of these cases show that the major metabolites are their corresponding sulfoxides (Ar–S(O)CF3) and sulfones (Ar–S(O)2CF3) [8][9]. Indeed, in the case of the insecticide fipronil it is actually the sulfoxide (Ar–S(O)CF3

Semi-synthesis and insecticidal activity of spinetoram J and its D-forosamine replacement analogues

• Kai Zhang,
• Jiarong Li,
• Honglin Liu,
• Haiyou Wang and
• Lamusi A

Beilstein J. Org. Chem. 2018, 14, 2321–2330, doi:10.3762/bjoc.14.207

• , P. R. China 10.3762/bjoc.14.207 Abstract Spinetoram, a mixture of spinetoram J (XDE-175-J, major component) and spinetoram L (XDE-175-L), is a new kind of fermentation-derived insecticide with a broad range of action against many insect pests, especially Cydia pomonella, Leaf miner and Thrips

• products with other groups, and the improved semi-synthesis will be helpful for further researches on spinetoram. Keywords: analogues; forosamine replacement; improved semi-synthesis; insecticide; natural products; spinetoram; Introduction Nowadays, insect pests are one of the primary hazards that affect

• crop production and storage, and pest control depends mainly on the use of insecticides. Therefore, it is particularly important to identify an efficient insecticide for controlling insect pests. In the quest for new and efficient insecticides, natural products have always been considered an excellent

A semisynthesis of 3'-O-ethyl-5,6-dihydrospinosyn J based on the spinosyn A aglycone

• Kai Zhang,
• Shenglan Liu,
• Anjun Liu,
• Hongxin Chai,
• Jiarong Li and
• Lamusi A

Beilstein J. Org. Chem. 2017, 13, 2603–2609, doi:10.3762/bjoc.13.257

• , Hohhot, China 10.3762/bjoc.13.257 Abstract Spinetoram, a mixture of 3'-O-ethyl-5,6-dihydrospinosyn J (XDE-175-J, major component) and 3'-O-ethylspinosyn L (XDE-175-L, minor component), is a novel kind of green and efficient insecticide with a broad range of action against various insects. Nowadays

• network (ANN)" to identify analogous molecules that might be effective to control fruit-tree pests, and then, spinetoram was discovered [13]. Although the structure of spinetoram is similar to that of spinosad, spinetoram has a broader spectrum of insecticide activity and more efficient performance in

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

• ). v) Reduction of the environmental toxicity The CDs can be used to minimize environmental pollution. As an example, in 1994, Loukas et al. reported the effect of γ-CD on dicyclopropylmethanone O-(diethoxyphosphoryl)oxime (named DCPE), a very active insecticide (Figure 4) [58]. The complexation of

Continuous flow nitration in miniaturized devices

• Amol A. Kulkarni

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

• preservative and also as an insecticide. 4-Amino-2-nitrophenol and 2-nitro-p-phenylenediamine are components of permanent hair dye products and fur dye. Several aniline derivatives are also used for the synthesis of various dyes [9], the first one being the aniline Yellow [10] reported in 1880. The history of

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

• Orgánica, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA, Córdoba, Argentina 10.3762/bjoc.9.14 Abstract An anhydrous 1:1 crystalline inclusion complex between the organophosphorus insecticide fenitrothion [O,O-dimethyl O-(3-methyl-4-nitrophenyl

• pesticide against undesired degradation reactions. Fenitrothion [O,O-dimethyl O-(3-methyl-4-nitrophenyl)phosphorothioate] (1, Figure 1) is an organophosphorus insecticide and acaricide [3]. It is effective against a wide range of pests that damage forests and various crops and it can also be used in the

• form of a residual contact spray to control flies, mosquitoes and cockroaches. Fenitrothion has also been employed in antimalarial programmes, where spraying of houses and animal shelters with this insecticide over extended periods significantly reduced the incidence and prevalence of the disease [4

Stereoselective synthesis of trans-fused iridoid lactones and their identification in the parasitoid wasp Alloxysta victrix, Part II: Iridomyrmecins

• Robert Hilgraf,
• Nicole Zimmermann,
• Lutz Lehmann,
• Armin Tröger and
• Wittko Francke

Beilstein J. Org. Chem. 2012, 8, 1256–1264, doi:10.3762/bjoc.8.141

• isolated from ants (Figure 1) [5] and along with some other volatile iridoids it has since been reported to be a potent insecticide and antibiotic from several natural sources [6]. Due to their challenging molecular structures and their interesting physiological properties, iridomyrmecins are attractive

Development of potential manufacturing routes for substituted thiophenes – Preparation of halogenated 2-thiophenecarboxylic acid derivatives as building blocks for a new family of 2,6-dihaloaryl 1,2,4-triazole insecticides

• John W. Hull Jr.,
• Duane R. Romer,
• David E. Podhorez,
• Mezzie L. Ash and
• Christine H. Brady

Beilstein J. Org. Chem. 2007, 3, No. 23, doi:10.1186/1860-5397-3-23

• the experimental insecticide target molecules XR-693 and XR-906 will be the topic of a forthcoming paper. Background Since the near world-wide ban on agricultural uses of the chlorinated insecticide DDT which began in the 1970's and 1980's, [1] the search for effective and safe insecticides that

• and inexpensive thiophene raw materials. Bromination Studies. Routes to 4-Bromo-3-methyl-2-thiophenecarbonyl chloride 1 Development of a viable commercial route to the insecticide XR-693 required a supply of 4-bromo-3-methyl-2-thiophenecarbonyl chloride 1 as a building block for attachment of the C

• -Trichloro-2-thiophenecarbonitrile, 3 Our investigation of synthetic routes to the 1,2,4-triazole insecticide XR-906 required a supply of the chlorinated thiophenes 2 or 3 as building blocks for attachment of the C-ring portion. Preparation of trichloro-2-thiophenecarbonitrile 3 has been reported starting