38930-22-2

Upstream product

• 576-26-1 2.6-dimethylphenol 
• 96-34-4 methyl chloroacetate 
• 96-32-2 bromoacetic acid methyl ester 
• 533-58-4 2-Iodophenol 
• 186395-08-4 methyl 2-(2-iodophenoxy)acetate 
• 616-38-6 carbonic acid dimethyl ester 

Downstream Products

• 35370-86-6 2-(2,6-Dimethyl-phenoxy)-thioacetamide 
• 115057-33-5 methyl 2,6-dimethyl-4-(4-methoxybenzoyl)phenoxyacetate 
• 68839-81-6 methyl 4-acetyl-2,6-dimethylphenoxyacetate 
• 64106-78-1 2-(2,6-dimethylphenoxy)acetohydrazide 
• 1572183-70-0 (E)-N’-((1H-indol-4-yl)methylene)-2-(2,6-dimethylphenoxy)acetohydrazide 
• 1572184-23-6 (E)-N’-((1H-indol-6-yl)methylene)-2-(2,6-dimethylphenoxy)acetohydrazide 
• 13335-71-2 2-(2,6-dimethylphenoxy)acetic acid 
• 115057-36-8 (4-Carboxymethoxy-3,5-dimethylphenyl)-4-methoxyphenylcarbinol 
• 189357-33-3 KNI-727 

Relevant academic research and scientific papers

Pd-Catalyzed ipso, meta-Dimethylation of ortho-Substituted Iodoarenes via a Base-Controlled C-H Activation Cascade with Dimethyl Carbonate as the Methyl Source

A methyl group can have a profound impact on the pharmacological properties of organic molecules. Hence, developing methylation methods and methylating reagents is essential in medicinal chemistry. We report a palladium-catalyzed dimethylation reaction of ortho-substituted iodoarenes using dimethyl carbonate as a methyl source. In the presence of K2CO3 as a base, iodoarenes are dimethylated at the ipso- and meta-positions of the iodo group, which represents a novel strategy for meta-C-H methylation. With KOAc as the base, subsequent oxidative C(sp3)-H/C(sp3)-H coupling occurs; in this case, the overall transformation achieves triple C-H activation to form three new C-C bonds. These reactions allow expedient access to 2,6-dimethylated phenols, 2,3-dihydrobenzofurans, and indanes, which are ubiquitous structural motifs and essential synthetic intermediates of biologically and pharmacologically active compounds.

N-ACYLHYDRAZONE DERIVATIVES FOR SELECTIVE T CELL INHIBITOR AND ANTI-LYMPHOID MALIGNANCY DRUG

The present invention relates to novel N-acylhydrazone derivatives, and more particularly to novel N-acylhydrazone derivatives having selective T cell inhibitory activity and/or anti-lymphoid malignancy activity, stereoisomers thereof, pharmaceutically acceptable salts thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, treatment methods using the compositions, and methods for preparing the novel N-acylhydrazone derivatives.

Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine

We designed and synthesized a new class of peptidomimetic human immunodeficiency virus (HIV) protease inhibitors containing a unique unnatural amino acid, allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy- 4-phenylbutyric acid], with a hydroxymethylcarbonyl (HMC) isostere as the active moiety. A systematic evaluation of structure - activity relationships for HIV protease inhibition, anti-HIV activities, and pharmacokinetic profiles has led to the delineation of a set of structural characteristics that appear to afford an orally available HIV protease inhibitor. Optimum structures, exemplified by 21f (JE-2147), incorporated 3-hydroxy-2- methylbenzoyl groups as the P2 ligand, (R)-5,5-dimethyl-1,3-thiazolidine-4- carbonyl (Dmt) residue at the P1' site, and 2-methylbenzylcarboxamide group as the P2' ligand. The present study demonstrated that JE-2147 has potent antiviral activities in vitro and exhibits good oral bioavailability and plasma pharmacokinetic profiles in two species of laboratory animals.

Synthesis of peptide amides by means of a solid phase method using acid-labile anchoring groups

The invention relates to new compounds of the formula STR1 in which R1 denotes (C1 -C8)-alkyl or optionally substituted (C6 -C14)-aryl, R2 denotes hydrogen or an amino acid residue which is