88072-12-2

Upstream product

• 88071-89-0 5-Methyl-2-nitro-benzoic acid tert-butyl ester 
• 2941-78-8 2-Amino-5-methylbenzoic acid 
• 503427-35-8 3-methyl-6-[(2,2,2-trifluoroacetyl)amino]benzoic acid 
• 75-65-0 tert-butyl alcohol 
• 940076-85-7 tert-butyl 5-methyl-2-(2,2,2-trifluoroacetamido)benzoate 

Downstream Products

• 88072-02-0 2-(3-Bromo-propionylamino)-5-methyl-benzoic acid tert-butyl ester 
• 1119085-73-2 2-(3'-chloro-2,4'-bipyridin-5-ylamino)-5-methylbenzoic acid 
• 1119085-49-2 5-methyl-2-(6-morpholinopyridin-3-ylamino)benzoic acid 
• 1119090-74-2 tert-butyl 2-(3'-chloro-2,4'-bipyridin-5-ylamino)-5-methylbenzoate 
• 1119090-57-1 tert-butyl 5-methyl-2-(6-morpholinopyridin-3-ylamino)benzoate 
• 1119091-71-2 tert-butyl 2-(6-bromopyridin-3-ylamino)-5-methylbenzoate 

Relevant academic research and scientific papers

A he west for favorable department method of preparation

The invention discloses a method for preparing cetilistat, which belongs to the technical field of the medicine preparation method, and is used for solving the problems of high three wastes, low yield and high cost in the current preparation method. The method comprises the following steps: 1)esterifying a compound A(2-amino-5-methyl benzoic acid) or its salt; 2) acylating an esterification object in the step 1) and chloroformic acid n-cetanol ester; 3)removing ester group of the compound obtained in the step 2) to obtain 2-(cetane carbonyl oxygen)amino-5-methyl benzoic acid; and 4)cyclizing the compound in the step 3) to obtain the target products. By improving the production steps, the invention provides the synthetic method with simple operation, high efficiency, and convenient industrial production for the cetilistat product.

AZABIPHENYLAMINOBENZOIC ACID DERIVATIVES AS DHODH INHIBITORS

New azabiphenylaminobenzoic acid derivatives having the chemcial structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH)

Substituted N-arylazetidinones, β-lactamases potential inhibitors

Two classes of substituted N-aryl azetidinones have been prepared by cyclization of various β-bromopropionanilides. The 7a class possess a carboxylic function in ortho, meta or para of the nitrogen and possibly another alkyl substituent on the aromatic nucleus. In the 7a class, the aromatic nucleus is substituted by a bromomethyl group instead of the alkyl one. Few of these azetidinones show a good affinity for various cell-free β-lactamases preparations, and thus are pretty good competitive inhibitors. Nevertheless, they do not act synergistically with ampicillin on β-lactamase producing bacterial strains. A poor antibacterial activity has been detected for few compounds. The azetidinones 7b which possess a latent electrophilic quinonimine methide function, do not give any progressive (suicide type) inhibition, or inactivation, of the enzymatic activity.