80194-72-5

Upstream product

• 80194-68-9 3-chloro-5-trifluoromethylpyridine-2-carboxylic acid 
• 79-37-8 oxalyl dichloride 

Downstream Products

• 128072-76-4 2-(3-chloro-5-trifluoromethylpyridin-2-ylcarbonyl)-cyclohex-1-en-1-ol-3-one 
• 1033463-30-7 3-chloro-5-(trifluoromethyl)picolinohydrazide 

Relevant academic research and scientific papers

Design, Synthesis, and Mechanism of Antiviral Acylurea Derivatives Containing a Trifluoromethylpyridine Moiety

Novel acylurea derivatives 7a-7ab were designed and synthesized by linking the active substructures trifluoromethylpyridine and anthranilic diamide via an acylurea bridge. Most of the title compounds exhibited good activity against tobacco mosaic virus (TMV), particularly compound 7x (EC50 of 211.8 μg/mL), which showed much higher curative activity than ningnanmycin (EC50 of 389.8 μg/mL), and compound 7ab, which showed excellent inactivation activity (EC50 of 36.1 μg/mL), similar to ningnanmycin (EC50 of 23.2 μg/mL). The preliminary mechanism of these derivatives was investigated. Autodocking analysis revealed that compounds 7x and 7ab had good affinity for TMV coat protein (TMV CP), with low binding energies (-7.86 and -8.59 kcal/mol) comparable to ningnanmycin (-8.75 kcal/mol). Molecular dynamics simulation showed that compound 7x had a stable system structure with a better binding free energy (-32.94 kcal/mol) than ningnanmycin (-25.62 kcal/mol). Microscale thermophoresis showed that compound 7x bound more strongly to TMV CP (Kd of 19.8 ± 7.3 μM) than ningnanmycin (Kd of 21.2 ± 7.3 μM). Transmission electron microscopy and self-assembly experiments demonstrated that compounds 7x and 7ab significantly obstructed the self-assembly of TMV RNA and TMV CP. This new acylurea derivative has excellent antiviral activity by targeting TMV CP and inhibiting TMV self-assembly and can be considered a candidate for antiviral applications.

Acyl thiourea and acyl urea derivatives containing trifluoromethylpyridine and application thereof

The invention discloses acyl thiourea and acyl urea derivatives containing trifluoromethylpyridine and an application thereof. A structure of the derivatives is shown in a general formula I. In the formula, definitions of R1, R2, R3, X and other groups are as shown in the description. The compound represented by the general formula I has excellent insecticidal activity, and can be used to preventand treat pests such as cotton bollworm, diamondback moth and brown planthopper, and can also be used to prevent and treat plant virus diseases such as TMV and CMV.

BACE1 INHIBITORS

The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

PYRIMIDINONE COMPOUND

A pyrimidinone compound represented by formula (1): wherein: A1 represents a nitrogen atom or a CR4; A2 represents a nitrogen atom and A3 represents a CR3b, or A2 represents a CR3a and A3 represents a nitrogen atom; Q represents an oxygen atom or a sulfur atom; G represents a C2-C10 chain hydrocarbon group having one or more halogen atoms, etc.; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms; R2 represents a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, etc.; R4 represents a hydrogen atom, etc.; R3, R3a, and R3b represent independently of each other a hydrogen atom, etc.; n represents 0, 1, or 2; and p represents 0, 1, 2, or 3 has an excellent efficacy for controlling harmful arthropods.

PYRIDINE DERIVATIVE OR ITS SALT, PESTICIDE CONTAINING IT AND PROCESS FOR ITS PRODUCTION

ABSTRACT: To provide a novel pesticide. The present invention provides a pesticide which contains, as an active ingredient, a novel pyridine derivative represented by the formula (I) or its salt: wherein R1? is alkyl, cycloalkyl, alkoxyalkyl or OR3?; R2? is 1H-1,2,4-triazol-1-yl which may be substituted, 1H-imidazol-1-yl which may be substituted, 1H-1,2,3-triazol-1-yl which may be substituted, or 4H-1,2,4-triazol-4-yl which may be substituted; X is alkyl which may be substituted, cycloalkyl which may be substituted, halogen, nitro, etc.; R3? is alkyl which may be substituted, cycloalkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, etc.; m is an integer of from 1 to 4.

Pyrazole derivatives as herbicides

Compounds of the following formula I wherein wherein all variables are as defined in the specification and the pyrazoleN-oxides, agrochemically acceptable salts and stereisomers thereof useful as herbisdes.

Novel herbicides

The invention relates to novel herbicidally active cyclohexanediones of formula I or I' STR1 in which R1 and R2 independently of one another are each hydrogen; halogen; nitro; cyano; C1 -C4 alkyl; C1 -C4 alkoxy; C1 -C4 alkyl-S(O)n --; COR8 ; C1 -C4 haloalkoxy; or C1 -C4 haloalkyl; R3, R4 and R5 independently of one another are each hydrogen; C1 -C4 alkyl; or phenyl or benzyl each unsubstituted or substituted by up to three identical or different substituents from halogen, nitro, cyano, C1 -C4 alkyl, C1 -C4 alkoxy, C1 -C4 alkyl-S(O)n --, C1 -C4 haloalkyl, C1 -C4 haloalkyl-S(O)n -- and C1 -C4 haloalkoxy; R6 is hydrogen; C1 -C4 alkyl, C1 -C4 alkoxycarbonyl; or cyano; R7 is OH; or O? M≈ ; R8 is OH; C1 -C4 alkoxy; NH2 ; C1 -C4 alkylamino; or di-C1 - C4 alkylamino; n is 0, 1 or 2; M+ is a cation equivalent of a metal ion or of an ammonium ion that is unsubstituted or substituted by up to three C1 -C4 alkyl, C1 -C4 hydroxyalkyl or C1 -C4 alkoxy-C1 -C4 alkyl groups, to herbicidal compositions, to processes for the preparation of novel compounds and to novel intermediates and the preparation thereof.