28168-48-1

Upstream product

• 3581-91-7 4,5-Dimethylthiazole 
• 100-52-7 benzaldehyde 
• 2353-46-0 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4,5-dimethyl-thiazolium; chloride 
• 3240-34-4 [bis(acetoxy)iodo]benzene 
• 6783-05-7 trans-2-phenylvinylboronic acid 
• 98-88-4 benzoyl chloride 
• 79247-96-4 4,5-dimethyl-thiazole-2-carboxylic acid ethyl ester 
• 79312-41-7 4,5-dimethylthiazole-2-carboxylic acid 

Relevant academic research and scientific papers

Discovery of Novel Pyrazole Carboxylate Derivatives Containing Thiazole as Potential Fungicides

Inspired by commercially established fluxapyroxad as the lead compound of novel efficient antifungal ingredients, novel pyrazole carboxylate derivatives containing a flexible thiazole backbone were successfully designed, synthesized, and detected for their in vitro and in vivo biological activities against eight agricultural fungi. The antifungal bioassay results showed that compound 24 revealed excellent bioactivities against Botrytis cinerea and Sclerotinia sclerotiorum, with median effective concentrations (EC50) of 0.40 and 3.54 mg/L, respectively. Compound 15 revealed remarkable antifungal activity against Valsa mali, with an EC50 value of 0.32 mg/L. For in vivo fungicide control against B. cinerea and V. mali, compounds 3 and 24 at 25 mg/L, respectively, displayed prominent efficacy on cherry tomatoes and apple branches. Molecular docking results demonstrated that compound 15 could form an interaction with several crucial residues of succinate dehydrogenase (SDH), and the in vitro enzyme assay indicated that the target compound 15 displayed an inhibitory effect toward SDH, with an IC50 value of 82.26 μM. The experimental results indicated that phenyl pyrazole carboxylate derivatives displayed a weak antifungal property and low activity compared to the other title substituent pyrazole carboxylate derivatives. Compounds 3, 15, and 24 are promising antifungal candidates worthy of further fungicide development due to their prominent effectiveness.

Photoinduced remote heteroaryl migration accompanied by cyanoalkylacylation in continuous flow

A photoinduced 1,4-heteroaryl migration from a carbon center to a nitrogen center accompanied by a cyanoalkylacylation of heterocyclic-substituted azidyl homoallylic alcohols and cycloketone oxime esters has been described. This simple and powerful protoc

N -Heterocyclic Carbene-Catalyzed Olefination of Aldehydes with Vinyliodonium Salts to Generate α,β-Unsaturated Ketones

An organocatalyzed metal-free, direct olefination of aldehydes with vinyliodonium salts has been achieved by an N-heterocyclic carbene-promoted C-H bond activation. The reaction proceeds under very mild conditions, delivering a range of (hetero)aryl-vinyl ketones in good yields. The retention of the double bond configuration is uniformly observed, and the application of 2-methoxyphenyl auxiliary group in iodonium salts secures a complete selectivity of the vinyl transfer.

Direct C-2 acylation of thiazoles with aldehydes via metal- and solvent-free c-h activation in the presence of tert-butyl hydroperoxide

A novel and efficient methodology for the synthesis of heteroaryl ketones by C-H activation of aldehydes and thiazoles is developed. The reaction occurs smoothly, under metal-, acid- and solvent-free conditions using tert-butyl hydroperoxide as the oxidant under an air atmosphere, to afford a wide range of heteroaryl ketones in moderate to good yields. The sp2 C-H bonds in the aldehyde and thiazole undergo direct oxidative cross-coupling, resulting in C-2 acylation of the azole. Georg Thieme Verlag Stuttgart · New York.

DMAP-catalyzed regel-type direct C-2 (Hetero)aroylation of oxazoles and thiazoles derivatives with acid chlorides

A Regel-type transition-metal-free direct C-2 aroylation of (benzo)oxazoles, (benzo)thiazoles and 1,3,4-oxadiazoles with acid chlorides catalyzed by N,N-dimethyl-4-aminopyridine (DMAP) is described. This methodology is effective with several aroyl and het