860465-22-1

Upstream product

• 1493-27-2 ortho-nitrofluorobenzene 
• 184368-89-6 1-iodo-2-(tert-butyldimethylsilyloxy)benzene 
• 533-58-4 2-Iodophenol 
• 609-73-4 o-nitroiodobenzene 

Downstream Products

• 869790-15-8 2-(2-iodophenoxy)aniline 
• 3158-85-8 10H-dibenzo[b,f][1,4]oxazepin-11-one 
• 1261604-62-9 2-(2-iodophenoxy)-N-methylaniline 
• 1370030-52-6 N-[2-(2-iodophenoxy)phenyl]acetamide 
• 1370030-54-8 N-[2-(2-iodophenoxy)phenyl]benzamide 
• 1370030-55-9 N-[2-(2-iodophenoxy)phenyl]-4-methylbenzenesulfonamide 
• 1370030-56-0 N-benzyl-2-(2-iodophenoxy)aniline 
• 135-67-1 phenoxazine 

Relevant academic research and scientific papers

Microwave assisted rapid synthesis of phenoxazines and benzopyridoxazines

A facile protocol for the synthesis of phenoxazines and benzopyridoxazines by Smiles rearrangement have been demonstrated in short reaction time under microwave irradiation. The control experiments suggest that a reaction proceeds through Smiles rearrangement followed SNAr ring closure by in situ cascade process. In our present work, both the electron donating and electron withdrawing groups were tolerant and provided a corresponding phenoxazine/benzopyridoxazine in good to moderate yields.

TRANSITION METAL COMPOUND, CATALYST FOR OLEFIN POLYMERIZATION AND METHOD FOR PRODUCING OLEFIN POLYMER

PROBLEM TO BE SOLVED: To provide a novel transition metal compound useful for a catalyst for olefin polymerization that shows superior performance in production of olefin polymers; for example, it has high polymerization activity and, in olefin copolymeri

Characterization of HJ-PI01 as a novel Pim-2 inhibitor that induces apoptosis and autophagic cell death in triple-negative human breast cancer

Aim: Pim-2 is a short-lived serine/threonine kinase, which plays a key role in metastasis of breast cancer through persistent activation of STAT3. Although the crystal structure of Pim-2 has been reported, but thus far no specific Pim-2-targeted compounds have been reported. In this study, we identified a novel Pim-2 inhibitor, HJ-PI01, by in silico analysis and experimental validation. Methods: The protein-protein interaction (PPI) network, chemical synthesis, molecular docking, and molecular dynamics (MD) simulations were used to design and discover the new Pim-2 inhibitor HJ-PI01. The anti-tumor effects of HJ-PI01 were evaluated in human breast MDA-MB-231, MDA-MB-468, MDA-MB-436, MCF-7 cells in vitro and in MDA-MB-231 xenograft mice, which were treated with HJ-PI01 (40 mg·kg-1 ·d-1, ig) with or without lienal polypeptide (50 mg·kg-1 ·d-1, ip) for 10 d. The apoptosis/autophage-inducing mechanisms of HJ-PI01 were elucidated using Western blots, immunoblots, flow cytometry, transmission electron microscopy and fluorescence microscopy. Results: Based on the PrePPI network, the potential partners interacting with Pim-2 in regulating apoptosis (160 protein pairs) and autophagy (47 protein pairs) were identified. Based on the structural characteristics of Pim-2, a total of 15 compounds (HJ-PI01 to HJ-P015) were synthesized, which showed moderate or remarkable anti-proliferative potency in the human breast cancer cell lines tested. The most effective compound HJ-PI01 exerted a robust inhibition on MDA-MB-231 cells compared with chlorpromazine and the pan-Pim inhibitor PI003. Molecular dynamics (MD) simulation revealed that HJ-PI01 had a good binding score with Pim-2. Moreover, HJ-PI01 (300 nmol/L) induced death receptor-dependent and mitochondrial apoptosis as well as autophagic death in MDA-MB-231 cells. In MDA-MB-231 xenograft mice, administration of HJ-PI01 remarkably inhibited the tumor growth and induced tumor cell apoptosis in vivo. Co-administration of HJ-PI01 with lienal polypeptide could improve the anti-tumor activity of HJ-PI01 and reduce its toxicity. Conclusion: The newly synthesized compound, HJ-PI01, can induce death receptor/mitochondrial apoptosis and autophagic cell death by targeting Pim-2 in human breast cancer cells in vitro and in vivo.

Transition-metal-free intramolecular N-arylations

N-Substituted phenoxazines and related aza analogs have been prepared from N-acetylated aryloxy anilides by transition-metal-free, base-catalyzed cyclization reactions. In the presence of a mixture of 10 mol % of N,N′-dimethylethylenediamine (DMEDA) and 2 equiv of K2CO 3 in toluene at 135 °C the products are obtained in high yields.

Palladium-catalyzed domino C-C/C-N coupling using a norbornene template: Synthesis of substituted benzomorpholines, phenoxazines, and dihydrodibenzoxazepines

A rapid, four-step approach to alkyl- and aryl-substituted benzomorpholines is accomplished by a Pd-catalyzed domino C-C/C-N bond coupling using a norbornene template. Extension to phenoxazines and dihydrodibenzoxazepines is presented.

Synthesis of dibenzo[ b, f ][1,4]oxazepin-11(10 H)-ones via intramolecular cyclocarbonylation reactions using PdI2/Cytop 292 as the catalytic system

Figure presented. The intramolecular cyclocarbonylation of substituted 2-(2-iodophenoxy)anilines was catalyzed by PdI2 and 1,3,5,7-tetramethyl-6-phenyl-2,4,8-trioxa-6-phospha-adamantane (Cytop 292) in an efficient manner. A series of substituted dibenzo[b,f][1,4]oxazepin-11(10H)- ones were prepared in good yields under mild reaction conditions.

RENIN INHIBITORS

Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.

RENIN INHIBITORS

Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.

RENIN INHIBITORS

Disclosed are compounds according to Formula (I): wherein the variables are defined herein. Such compounds are can bind aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic pro

PIPERIDINE AND MORPHOLINE RENIN INHIBITORS

Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.