42174-78-7

Upstream product

• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 
• 16588-34-4 4-chloro-3-nitro-benzaldehyde 
• 5551-11-1 4-Chloro-2-nitrobenzaldehyde 
• 105-36-2 ethyl bromoacetate 
• 64-17-5 ethanol 
• 20797-48-2 (E)-4-chloro-3-nitrocinnamic acid 

Downstream Products

• 328899-08-7 (E)-3-(4-Chloro-3-nitro-phenyl)-prop-2-en-1-ol 
• 24364-03-2 ethyl 4-amino-3-nitrocinnamate 
• 223577-08-0 1-Chloro-4-((E)-3-chloro-propenyl)-2-nitro-benzene 

Relevant academic research and scientific papers

Polyethyleneimine-Supported Triphenylphosphine and Its Use as a Highly Loaded Bifunctional Polymeric Reagent in Chromatography-Free One-Pot Wittig Reactions

A polyethyleneimine-supported triphenylphosphine reagent has been synthesized and used as a highly loaded bifunctional homogeneous reagent in a range of one-pot Wittig reactions that afforded high yields of the desired products after simple purification procedures. The approach also served efficiently in tandem reaction sequences involving a one-pot Wittig reaction followed by conjugate reduction of the newly formed alkene product in situ. In these transformations, the phosphine oxide groups generated in the Wittig reaction served as the catalyst for activating trichlorosilane in the subsequent reduction reaction.

Structure-based design of potent and selective leishmania N -myristoyltransferase inhibitors

Inhibitors of Leishmania N-myristoyltransferase (NMT), a potential target for the treatment of leishmaniasis, obtained from a high-throughput screen, were resynthesized to validate activity. Crystal structures bound to Leishmania major NMT were obtained,

Chromatography-free wittig reactions using a bifunctional polymeric reagent

The first example of a polystyrene bearing two distinct reagent groups has been prepared. This phosphine and amine functionalized material was used in one-pot Wittig reactions with an aldehyde and either an α-halo-ester, -ketone, or -amide. Due to the heterogeneous nature of the polymer, the desired alkene product of these reactions could be isolated in excellent yield in essentially pure form after only filtration and solvent removal.

Hapten Synthesis and Antibody Development for Polychlorinated Dibenzo-p-dioxin Immunoassays

This paper reports the synthesis of haptens and the generation and preliminary evaluation of polyclonal antibodies for the detection of dioxins such as TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) by ELISA (enzyme-linked immunosorbent assay). These novel haptens contain unsaturation between the halogenated dibenzo-p-dioxin ring system and the protein to which it is conjugated, presenting a rigid handle structure. The substitution pattern is identical with or similar to that of TCDD (i.e., 2,3,7,8- or 1,2,3,7,8-). Finally, the haptens lack polar groups for hydrogen bonding. In direct binding assays using the new polyclonal antibodies there was excellent recognition of hapten-protein conjugates, including recognition of those hapten conjugates that were not used as immunogens (i.e., assay systems heterologous in hapten structure). These haptens do elicit selective immune responses in rabbits. Their evaluation in an ELISA format demonstrated the usefulness of these haptens for the detection of dioxins. An IC50 of 0.8 ng/well (16 ng/mL) was observed for an unoptimized system that used 2,3,7-trichloro-8-methyldibenzo-p-dioxin as an analytical surrogate standard.

Synthesis and μ-opioid receptor affinity of a new series of nitro substituted 3,8-diazabicyclo[3.2.1]octane derivatives

A new series of analogues (1c-j; 2c-i) of the previously reported analgesic 3,8-diazabicyclo[3.2.1]octanes (1a,b; 2a,b) was synthesized and tested for their affinity towards μ-opioid receptors. Modifications were introduced either at the cinnamyl or the acyl side chains. The majority of the new compounds, with the exception of 1c,j and 2c, showed K(i) values better or comparable with those of the models.

Receptor-based design of novel dihydrofolate reductase inhibitors: Benzimidazole and indole derivatives

Although many thousands of inhibitors of the enzyme dihydrofolate reductase (DHFR) have been synthesized, all of the very active compounds have been 2,4-diaminopyrimidines or very close analogues. This paper describes 2,4-diamino-6-benzylbenzimidazole (3b