89840-66-4

Upstream product

• 5455-59-4 2-Nitrobenzenesulfonamide 
• 27350-45-4 (S)-sec-butyl diphenylphosphinite 
• 33966-50-6 SEC-BUTYLAMINE 
• 1694-92-4 2-Nitrobenzenesulfonyl chloride 
• 27350-45-4 sec-butyl diphenylphosphinite 
• 13250-12-9 (R)-sec-butylamine 

Relevant academic research and scientific papers

An efficient method for the preparation of N-alkylamides from alkyl diphenylphosphinites and amides by using methyl acrylate

N,N-Dibenzyltrifluoroacetamide was formed in good yield by treating benzyl diphenylphosphinite with N-benzyltrifluoroacetamide in the presence of easily available methyl acrylate under mild conditions. Yields obtained for the corresponding inverted sulfon

An efficient method for the preparation of monoalkylated sulfonamides from unsubstituted sulfonamides and alkyl diphenylphosphinites by oxidation-reduction condensation using trimethylsilylmethyl azide

An efficient method for monoalkylation of unsubstituted sulfonamides was established by using alkyl diphenylphosphinites, sulfonamides and trimethylsilylmethyl azide and the monoalkylated sulfonamides were afforded in good yields under neutral conditions.

Chemokine receptor binding heterocyclic compounds

This invention relates to a novel class of heterocyclic compounds that bind chemokine receptors, inhibiting the binding of their natural ligands thereby. These compounds result in protective effects against infection by HIV through binding to chemokine receptors, including CXCR4 and CCR5, thus inhibiting the subsequent binding by these chemokines. The present invention provides a compound of Formula I wherein, W is a nitrogen atom and Y is absent or, W is a carbon atom and Y═H; R1to R7may be the same or different and are independently selected from hydrogen or straight, branched or cyclic C1-6alkyl; R8is a substituted heterocyclic group or a substituted aromatic group Ar is an aromatic or heteroaromatic ring each optionally substituted at single or multiple, non-linking positions with electron-donating or withdrawing groups; n and n′ are independently, 0-2; X is a group of the formula: Wherein, Ring A is an optionally substituted, saturated or unsaturated 5 or 6-membered ring, and P is an optionally substituted carbon atom, an optionally substituted nitrogen atom, sulfur or oxygen atom. Ring B is an optionally substituted 5 to 7-membered ring. Ring A and Ring B in the above formula can be connected to the group W from any position via the group V, wherein V is a chemical bond, a (CH2)n″group (where n″=0-2) or a C═O group. Z is, (1) a hydrogen atom, (2) an optionally substituted C1-6alkyl group, (3) a C0-6alkyl group substituted with an optionally substituted aromatic or heterocyclic group, (4) an optionally substituted C0-6alkylamino or C3-7cycloalkylamino group, (5) an optionally substituted carbonyl group or sulfonyl. These compounds further include any pharmaceutically acceptable acid addition salts and metal complexes thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof.

Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists

1-((1R,2R)-2-Hydroxy-1-methyl-2-phenylethyl)-1-methyl-3-(4-phenoxyphenyl)urea (1) was identified as a hit from the screening of the neuropeptide Y5 (NPY5) receptor. This lead was optimized for in vitro potency by changing the stereochemistry, the phenylethyl segment, the urea portion, and the 4-phenoxyphenyl group on the molecule. Over 40 analogues of 1 were prepared to study the structure-activity relationship for this series. The most potent compounds in this class have IC50S less than 0.1 nM at the NPY5 receptor (e.g., 40f, 44a, and 47). To determine the functional activity for this series of compounds, selected analogues were tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor. All urea analogues tested in the functional assay acted as antagonists (e.g., 1, 32, 40a, and 44e).