64448-50-6

Upstream product

• 860521-46-6 thiobenzoic acid-(3-nitro-anilide) 
• 4771-08-8 N-(3-nitrophenyl)benzamide 
• 51657-41-1 5,5'-dinitro-2,2'-disulfanediyl-bis-aniline 
• 10403-47-1 2-bromo 5-nitroaniline 
• 98-88-4 benzoyl chloride 
• 6283-25-6 H₂NC₆H₃(Cl)NO₂ 
• 205827-96-9 N-(2-chloro-5-nitro-phenyl)-benzamide 
• 873984-37-3 bis-(2-benzoylamino-4-nitro-phenyl)-disulfide 
• 737765-82-1 N-(2-bromo-5-nitrophenyl)benzamide 
• 1372687-96-1 1-[N-(2-chloro-5-nitro-phenyl)-benzimidoyl]3-(4-methoxy phenyl) thiourea 
• 1372687-94-9 1-[N-(2-chloro-5-nitro-phenyl)-benzimidoyl] 3-(4-methyl phenyl) thiourea 
• 7686-29-5 2-amino-4-nitrobenzenethiol 

Downstream Products

• 13399-20-7 2,7-diphenyl-benzo[1,2-d;3,4-d']bisthiazole 
• 43087-91-8 2-phenyl-1,3-benzothiazol-5-amine 

Relevant academic research and scientific papers

Method used for rapid preparation of benzo-heterocycle compound with physical grinding under solvent-free room temperature conditions

The invention discloses a method used for rapid preparation of benzo-heterocycle compound with physical grinding under solvent-free room temperature conditions. According to the method, glacial aceticacid is taken as a catalyst; at solvent-free room temperature conditions, physical grinding is adopted, reaction of 2-substituted arylamines (2-mercapto arylamine, 2-aminophenol, and o-phenylenediamine) and aromatic aldehydes is carried out using physical grinding. The method is friendly to the environment, is simple in operation, is safe, is low in cost, and is high in efficiency. Compared withthe prior art, the advantages are that: the method is suitable for a large amount of functional groups, yield is high, less by-product is generated, operation is simple, the method is safe, cost is low, and the method is friendly to the environment.

Method for preparing benzothiazole compound through microwave catalysis in water phase

The invention discloses a method for preparing a benzothiazole compound through/under microwave catalysis in a water phase. A water-soluble coordination compound is used as a catalyst, and a reactionof inorganic sulfide, 2-iodoaniline and aldehyde is efficiently catalyzed through microwaves in a pure water phase. The method for preparing the benzothiazole compound is environmentally friendly, convenient to operate, safe, cheap and efficient. Compared with the prior art, the method is applied to a large quantity of functional groups, high in yield, simple to operate, safe, low in cost and environmentally friendly and produces a few byproducts.

Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis

A previous publication from this lab (Patrick, et al. Bioorg. Med. Chem. 2016, 24, 2451-2465) explored the antitrypanosomal activities of novel derivatives of 2-(2-benzamido)ethyl-4-phenylthiazole (1), which had been identified as a hit against Trypanosoma brucei, the causative agent of human African trypanosomiasis. While a number of these compounds, particularly the urea analogues, were quite potent, these molecules as a whole exhibited poor metabolic stability. The present work describes the synthesis of 65 new analogues arising from medicinal chemistry optimization at different sites on the molecule. The most promising compounds were the urea derivatives of 2-aryl-benzothiazol-5-amines. One such analogue, (S)-2-(3,4-difluorophenyl)-5-(3-fluoro-N-pyrrolidylamido)benzothiazole (57) was chosen for in vivo efficacy studies based upon in vitro activity, metabolic stability, and brain penetration. This compound attained 5/5 cures in murine models of both early and late stage human African trypanosomiasis, representing a new lead for the development of drugs to combat this neglected disease.

COMPOUNDS FOR TREATMENT OF TRYPANOSOMES AND NEUROLOGICAL PATHOGENS AND USES THEREOF

The present invention relates to novel compounds that cross the blood-brain barrier and are effective inhibitors of neurological pathogens such as trypanosomes. The invention further relates to the use of these compounds for treating disorders related to trypanosomes and neurological pathogens.

Syntheses and reactivity of alkyl 1-[ N-(2-chloro-5-nitro-phenyl)- benzimidoyl] thioureas

A series of new alkyl 1-[N-(2-chloro-5-nitro-phenyl)-benzimidoyl] thioureas 3a-h were prepared from benzamides 1a-c. Benzimidoyl thioureas 3a-e afforded 5-nitro-2-phenyl-benzothiazole 5a-c under basic conditions via thiourea-isothiourea rearrangement and SNAr. A mechanistic rationalization supported by the direct formation of benzothioamide 8 and bis-benzimidoyl sulfide 9 derivatives from the reaction of imidoyl isothiocyanate 2 with bulky amines was supported.

4,5-azolo-oxindoles

Disclosed are novel 4,5-azolo-oxindoles having the formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.