14056-07-6

Upstream product

• 90-01-7 salicylic alcohol 
• 64-17-5 ethanol 
• 7553-56-2 iodine 
• 90-02-8 salicylaldehyde 
• 119-30-2 2-hydroxy-5-iodobenzoic acid 
• 1761-62-2 5-iodosalicyclaldehyde 
• 888958-33-6 6-iodo-2,2-dimethylbenzo[1,3]dioxin-4-one 
• 540-38-5 p-Iodophenol 
• 133-91-5 3,5-diiodosalicylic acid 

Downstream Products

• 1761-62-2 5-iodosalicyclaldehyde 
• 910898-53-2 (2-hydroxy-5-iodobenzyl)(triphenyl)phosphonium bromide 
• 910898-55-4 2-(4-fluorophenyl)-5-(phenylthio)-1-benzofuran 
• 910898-54-3 2-(4-fluorophenyl)-5-iodo-1-benzofuran 
• 1243682-24-7 4-(2-chloroethyl)-2-(2-hydroxy-5-iodobenzyl)phenol 

Relevant academic research and scientific papers

A Modular Synthesis of Teraryl-Based α-Helix Mimetics, Part 3: Iodophenyltriflate Core Fragments Featuring Side Chains of Proteinogenic Amino Acids

Teraryl-based α-helix mimetics have proven to be useful compounds for the inhibition of protein-protein interactions (PPI). We have developed a modular and flexible approach for the synthesis of teraryl-based α-helix mimetics using a benzene core unit featuring two leaving groups of differentiated reactivity in the Pd-catalyzed cross-coupling used for teraryl assembly. In previous publications we have introduced the methodology of 4-iodophenyltriflates decorated with the side chains of some of the proteinogenic amino acids. We herein report the core fragments corresponding to the previously missing amino acids Arg, Asn, Asp, Met, Trp and Tyr. Therefore, our set now encompasses all relevant amino acid analogues with the exception of His. In order to be compatible with the triflate moiety, some of the nucleophilic side chains had to be provided in a protected form to serve as stable building blocks. Additionally, cross-coupling procedures for the assembly of teraryls were investigated.

Development of chemical probes: Toward the mode of action of a methylene-linked di(aryl acetate) E1

Analogues of the novel inhibitor of the PI3-K/PKB pathway, 2-[5-(2-chloroethyl)-2-acetoxy-benzyl]-4-(2-chloroethyl)-phenyl acetate (E1), have been prepared and preliminary SAR performed. This established that at least one of the chloroethyl para-substituents could be removed or modified and the ability to inhibit PKB/Akt activation retained. Synthetic methodologies were then developed to methylene-linked aryl acetates for use as molecular probes to identify the target of compound E1.

Chemoselective reduction of aldehydes using decaborane in aqueous solution

Reduction of aldehydes using decaborane (B10H14) in an aqueous solution gave the corresponding alcohol chemoselectively in good to high yields. Copyright Taylor & Francis Group, LLC.

ARYLSULFONYL BENZOFUSED HETEROCYCLES AS 5-HT2A ANTAGONISTS

Compounds of formula (I): are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various CNS disorders.

Efficient and selective reduction protocols of the 2,2-dimethyl-1,3- benzodioxan-4-one functional group to readily provide both substituted salicylaldehydes and 2-hydroxybenzyl alcohols

Two complementary procedures have been developed that selectively allow for the synthesis of either substituted salicylaldehydes or the corresponding 2-hydroxylbenzyl alcohols upon treatment of the 2,2-dimethyl-1,3-benzodioxan-4- one functional group with DIBAL-H or LAH, respectively.

Substituted benzopyran derivatives for the treatment of inflammation

A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.

Substituted benzopyran analogs for the treatment of inflammation

A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.