294665-21-7

Upstream product

• 609-67-6 2-Iodobenzoyl chloride 
• 6306-52-1 L-valine methylester hydrochloride 
• 4070-48-8 L-Valine methyl ester 
• 88-67-5 2-Iodobenzoic acid 

Downstream Products

• 353764-08-6 (S)-2-[(2-iodobenzoyl)amino]-3-methyl-1-butanol 
• 294665-27-3 N-(2-iodobenzoyl) valine 
• 1208130-66-8 N-((S)-1-((S)-1-(hydroxyamino)-5-(3-nitroguanidino)-1-oxopentan-2-ylamino)-3-methyl-1-oxobutan-2-yl)-2-iodobenzamide 
• 353764-11-1 (S,E)-methyl 4-[(2-iodobenzoyl)amino]-5-methyl-2-hexenoate 

Relevant academic research and scientific papers

A Convenient 5-exo-dig Cyclization Route to Diastereomerically Pure Methyl (2S)-2-(1-benzyl-3-oxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylbutanoate

[Figure not available: see fulltext.] A robust method toward the synthesis of diastereomerically pure methyl (2S)-2-(1-benzyl-3-oxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylbutanoate has been described. The key reactions in the synthesis are: HATU-mediated coupling, Pd-catalyzed Sonogashira coupling, base-mediated 5-exo-dig cyclization, and catalytic hydrogenation. The diastereomeric mixture is subjected to trituration with heptane to furnish both diastereomers in moderate yields. The relative stereochemistry was confirmed by the single crystal X-ray diffractometry. The key feature of the method is the simplicity of the diastereomeric separation.

Novel L-arginine derivatives as aminopeptidase N inhibitors: design, chemistry, and pharmacological evaluation

Considering the important roles played in tumor, aminopeptidase N has been an appealing target for anti-tumor drug development. Here, a serial of novel aminopeptidase N inhibitors with L-arginine scaffold were designed, synthesized and evaluated for aminopeptidase N inhibitory activities. The preliminary anti-enzyme activity assay demonstrated that compounds 5e, 5h, 11e, 11g, and 11h showed comparable activities with the positive control bestatin, an approved aminopeptidase N inhibitor. In vitro anti-proliferation assay, compound 5f showed excellent activities against four kinds of tumor cells which overexpress aminopeptidase N. In vivo anti-metastasis assay, compounds 5f and 11g exhibited better activities than bestatin. So 5f and 11g should be lead compounds as novel aminopeptidase N inhibitors for further development.

Design, synthesis and primary activity assay of bi- or tri-peptide analogues with the scaffold l-arginine as amino-peptidase N/CD13 inhibitors

A series of bi- or tri-peptide analogues with the scaffold l-arginine were designed, synthesized and evaluated for their inhibitory activities against amino-peptidase N (APN) and metalloproteinase-2 (MMP-2). The primary activity assay showed that all the compounds exhibited higher inhibitory activities against APN than MMP-2. Within this series, compounds C6 and C7 (IC50 = 4.2 and 4.3 μM) showed comparable APN inhibitory activities with the positive control bestatin (IC50 = 3.8 μM).

Highly effective, easily accessible screw-sense-determining end group in the asymmetric polymerization of 1,2-diisocyanobenzenes

Enantiopure helical poly(quinoxaline-2,3-diyl) was formed stereoselectively in the polymerization of 1,2-diisocyanobenzene using a new organopalladium initiator bearing the (4S,5S)-N-acyl-4,5-dihydro-4,5-diphenyl-1H-imidazol-2-yl group as the polymer-end screw-sense-determinant.

Efficient Synthesis of Chiral Isoquinoline and Pyrido[1,2-b]-isoquinoline Derivatives via Intramolecular Heck Reactions

The palladium(0)-catalyzed reaction of derivatives of γ-amino-α,β-unsaturated esters bearing an N-(2-iodobenzoyl) substituent results in an intramolecular Heck reaction, the outcome of which depends on the structure of the substrate as well as on the expe

Synthesis and reactions of amino acid-derived benziodazole oxides: New chiral oxidizing reagents

The novel benziodazole oxides (3) can be prepared by oxidation of the readily available 2-iodobenzamides (5 or 6) with potassium bromate. Benziodazole oxides can find practical application as selective oxidizing reagents analogous to the widely used Dess-