34810-84-9

Upstream product

• 40545-33-3 2-amino-5-methylbenzamide 
• 4692-99-3 6-methyl-1H-benzo[d][1,3]oxazine-2,4-dione 
• 74-89-5 methylamine 
• 2941-78-8 2-Amino-5-methylbenzoic acid 
• 608-05-9 5-methyl-indole-2,3-dione 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 3113-72-2 5-methyl-2-nitrobenzoic acid 
• 20877-81-0 5-methyl-1H-benzo[d][1,3]oxazine-2,4-dione 

Downstream Products

• 1022969-64-7 2-(2,5-dichloro-pyrimidin-4-ylamino)-5,N-dimethyl-benzamide 

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.

Green synthesis of novel phosphonate derivatives using ultrasonic irradiation

[Figure not available: see fulltext.] A novel and efficient procedure for the generation of quinazolinone phosphonate derivatives employing the reaction of euparin, isatin or its derivatives, primary amines, dialkyl acetylenedicarboxylates, trimethyl phosphite or triphenyl phosphite, and acidic solution of hydrogen peroxide in aqueous media at ambient temperature under ultrasonic irradiation was developed. Without ultrasonic irradiation, the reaction does not proceed and agitation of the reaction mixture is difficult. Some advantages of this procedure are: short time of reaction, high yields of products, easy isolation of products.

Diversification of quinazolinones by Pd-catalyzed C(sp3)-acetoxylation

The quinazolinone ring has been exploited as a directing group for C(sp3)-H functionalization for the first time. The proximal C-γ(sp3)-H bonds have been oxidized by palladium-catalyzed acetoxylation reaction. Various functional grou

Synthetic method of 2-amino-4-bromo-N,5-dimethyl benzamide

The invention discloses a synthetic method of 2-amino-4-bromo-N,5-dimethyl benzamide, and belongs to the field of chemical synthesis. The synthetic method comprises the following steps: firstly, by taking 2-nitro-5-methyl benzoic acid as a raw material and using ferric chloride hexahydrate and palladium as a composite catalyst, adding the materials into hydrazine hydrate solution and performing reduction reaction to obtain 2-amino-5-methyl benzoic acid; adding the 2-amino-5-methyl benzoic acid and dichloromethane into bis(trichloromethyl) carbonate tetrahydrofuran solution by taking pyridine as a catalyst, and performing cyclization reaction; after the reaction is ended, performing microwave heating to reflux; after reflux, adding methylamine water solution and performing amination reaction to obtain 2-amino-N,5-dimethyl benzamide; finally, enabling the 2-amino-N,5-dimethyl formamide, hydrogen peroxide and hydrobromic acid solution to perform halogenating reaction, thus obtaining the 2-amino-4-bromo-N,5-dimethyl benzamide.

Mechanistic insights into a catalyst-free method to construct quinazolinones through multiple oxidative cyclization

A novel one-pot benign oxidative cyclization of alcohols with 2-aminobenzamides was successfully developed without catalyst to afford the quinazolinones under O2. This one-pot protocol involved oxidations and cyclizations to construct the skeleton of quinazolinones through possibly three kinds of distinct reaction mechanisms.

PYRIDINE COMPOUNDS

The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.

FUSED BICYCLIC DERIVATIVES OF 2,4-DIAMINOPYRIMIDINE AS ALK AND C-MET INHIBITORS

The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.