41994-44-9

Upstream product

• 2516-95-2 5-chloro-2-nitrobenzoic acid 
• 108-88-3 toluene 

Downstream Products

• 51282-49-6 methyl 5-chloro-2-nitrobenzoate 
• 40763-96-0 2-nitro-5-chlorobenzamide 
• 480451-75-0 5-chloro-N,N-dimethyl-2-nitrobenzamide 
• 219487-62-4 5-chloro-2-nitro-N-phenylbenzamide 
• 57487-53-3 C₂₂H₁₅Cl₃N₆O₃ 
• 63931-30-6 2-[(5-Chloro-2-nitro-benzoyl)-ethyl-amino]-malonic acid diethyl ester 
• 22978-10-5 5-Chloro-N-cyanomethyl-2-nitro-benzamide 
• 18640-60-3 5-chloro-2-nitroacetophenone 
• 63931-28-2 2-[(5-Chloro-2-nitro-benzoyl)-methyl-amino]-malonic acid diethyl ester 
• 144485-99-4 5-Chloro-N-(3-methyl-isoxazol-5-yl)-2-nitro-benzamide 
• 87693-25-2 5-chloro-2-nitro-N-1H-tetrazol-5-ylbenzamide 
• 149490-10-8 5-Chloro-N-(2-chloro-pyridin-3-yl)-2-nitro-benzamide 
• 111054-11-6 3-(5-Chloro-2-nitro-phenyl)-3-oxo-2-(triphenyl-λ⁵-phosphanylidene)-propionic acid tert-butyl ester 
• 87857-67-8 diethyl 5-chloro-2-nitrobenzoylaminomalonate 

Relevant academic research and scientific papers

Covalent Occlusion of the RORγt Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site

The nuclear receptor RORγt is a key positive regulator in the differentiation and proliferation of T helper 17 (Th17) cells and the production of proinflammatory cytokines like IL-17a. Dysregulation of this pathway can result in the development of various

Practical and Scalable Manufacturing Process for Plasma Kallikrein Inhibitor ASP5069

The plasma kallikrein inhibitor ASP5069 is a promising drug candidate for the treatment of edema and hematoma and for the prevention of bleeding during surgery. Here, we report the development of a practical and scalable process for manufacturing ASP5069

METHOD FOR PRODUCING DICARBOXYLIC ACID COMPOUND

It is an object of the present invention to provide an excellent method for producing an excellent therapeutic agent. The solution of the present invention is as shown in the following scheme: wherein R1 represents a C1-C6 alkyl group, R2 represents a C1-C6 alkyl group, and R3 represents a C1-C6 alkyl group.

Anthranilamide-based 2-phenylcyclopropane-1-carboxamides, 1,1'-biphenyl-4-carboxamides and 1,1'-biphenyl-2-carboxamides: Synthesis biological evaluation and mechanism of action

Several anthranilamide-based 2-phenylcyclopropane-1-carboxamides 13a-f, 1,1’-biphenyl-4-carboxamides 14a-f and 1,1’-biphenyl-2-carboxamides 17a-f were obtained by a multistep procedure starting from the (1S,2S)-2-phenylcyclopropane-1-carbonyl chloride 11, the 1,1'-biphenyl-4-carbonyl chloride 12 or the 1,1'-biphenyl-2-carbonyl chloride 16 with the appropriate anthranilamide derivative 10a-f. Derivatives 13a-f, 14a-f and 17a-f showed antiproliferative activity against human leukemia K562?cells. Among these derivatives 13b, 14b and 17b exerted a particular cytotoxic effect on tumor cells. Derivative 17b showed a better antitumoral effect on K562?cells than 13b and 14b. Analyses performed to explore 17b mode of action revealed that it induced an arrest in G2/M phase of cell cycle which was consequent to DNA lesions as demonstrated by the increase in phospho-ATM and γH2AX, two known markers of DNA repair response system. The effect of 17b was also related to ROS generation, activation of JNK and induction of caspase-3 dependent apoptosis.

NOVEL SULFONYLAMINOBENZAMIDE COMPOUNDS AS ANTHELMINTICS

The present invention relates to a new compound of formula (I) wherein the variables have the meaning as indicated in the claims; or an enantiomer or salt thereof. The compounds of formula (I) are useful in the control of parasites, in particular endopara

Synthesis and anticancer activity of 2-aryl-6-diethylaminoquinazolinone derivatives

A series of 6-diethylaminoquinazolin-4(3H)-ones with bulky aryl rings at C2 were designed to cover the vacant space of ligand binding pocket of topoisomerase (topo) I-DNA complex. The desired derivatives were synthesized by thermal cyclodehydration/dehydr

Copper-Catalyzed Domino Reaction Involving Nitro as an Unexpected Leaving Group: Construction of Dibenzo-Fused Azepinone Ring

A copper-catalyzed new domino reaction allowed the facile and direct construction of the dibenzo-fused azepinone ring leading to an array of novel small molecules. The co-catalyst, ligand or additive free one-pot method afforded a unique class of function

New compounds

The present invention relates to a new compound of formula wherein the variables have the meaning as indicated in the claims; or an enantiomer or salt thereof. The compounds of formula (I) are useful in the control of parasites, in particular endoparasite

Structure-activity relationships for lipoprotein lipase agonists that lower plasma triglycerides in vivo

The risk of cardiovascular events increases in individuals with elevated plasma triglyceride (TG) levels, therefore advocating the need for efficient TG-lowering drugs. In the blood circulation, TG levels are regulated by lipoprotein lipase (LPL), an unstable enzyme that is only active as a non-covalently associated homodimer. We recently reported on a N-phenylphthalimide derivative (1) that stabilizes LPL in vitro, and moderately lowers triglycerides in vivo (Biochem. Biophys. Res. Commun. 2014, 450, 1063). Herein, we establish structure-activity relationships of 51 N-phenylphthalimide analogs of the screening hit 1. In vitro evaluation highlighted that modifications on the phthalimide moiety were not tolerated and that lipophilic substituents on the central phenyl ring were functionally essential. The substitution pattern on the central phenyl ring also proved important to stabilize LPL. However, in vitro testing demonstrated rapid degradation of the phthalimide fragment in plasma which was addressed by replacing the phthalimide scaffold with other heterocyclic fragments. The in vitro potency was retained or improved and substance 80 proved stable in plasma and efficiently lowered plasma TGs in vivo.

Nucleophilic ring-opening of benzoxazinones by DBU: Some observations

This communication demonstrates the formation of an unusual nucleophilic ring opening of benzoxazinones by 1,8-diazabicycloundec-7-ene (DBU). This observation contradicts the intrinsic feature of a hindered nonnucleophilic base like DBU. Confirmation of t