761440-22-6

Usage

Uses

Used in Pharmaceutical Industry:
1-(3-Methoxy-4-nitrophenyl)piperidin-4-ol is used as a building block for the synthesis of various pharmaceuticals due to its versatile chemical structure and potential pharmacological properties. It serves as a key component in the development of new drugs, contributing to the advancement of medicinal chemistry and drug discovery.
Used in Organic Compounds Synthesis:
In the field of organic chemistry, 1-(3-Methoxy-4-nitrophenyl)piperidin-4-ol is utilized as a starting material for the synthesis of a range of organic compounds. Its unique structure allows for the creation of diverse chemical entities, expanding the scope of chemical research and applications.

InChI:InChI=1/C12H16N2O4/c1-18-12-8-9(2-3-11(12)14(16)17)13-6-4-10(15)5-7-13/h2-3,8,10,15H,4-7H2,1H3

Upstream product

• 5382-16-1 4-HYDROXYPIPERIDINE 
• 448-19-1 4-fluoro-2-methoxy-1-nitrobenzene 

Downstream Products

• 761440-64-6 1-(3-methoxy-4 nitrophenyl)piperidin-4-one 
• 761440-87-3 1-(4-amino-3-methoxyphenyl)piperidin-4-ol 
• 761440-66-8 4-(2-ethoxy-ethoxy)-1-(3-methoxy-4-nitro-phenyl)-piperidine 
• 1356962-95-2 N-cyclopropyl-1-(3-methoxy-4-nitrophenyl)piperidin-4-amine 
• 1089279-90-2 1-(3-methoxy-4-nitrophenyl)-N,N-dimethylpiperidine-4-amine 
• 1089279-91-3 1-(4-amino-3-methoxyphenyl)-N,N-dimethylpiperidine-4-amine 
• 761440-65-7 1-(1-(3-methoxy-4-nitrophenyl)piperidin-4-yl)-4-methylpiperazine 
• 1197953-54-0 5-chloro-N⁴-[2-(dimethylphosphonyl)phenyl]-N²-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidine-2,4-diamine 

Relevant academic research and scientific papers

Brigatinib intermediate, salt thereof, preparation method thereof and preparation method of brigatinib

The invention relates to the technical field of chemical synthesis, and particularly discloses a brigatinib intermediate, salt and a preparation method thereof, and a preparation method of brigatinib.The structural formula of the brigatinib intermediate i

PYRIMIDINE DERIVATIVE AND USE THEREOF

The present invention provides a pyrimidine derivative and a use thereof. The pyrimidine derivative is the compound shown in formula I or a pharmaceutically acceptable salt, hydrate, solvate, metabolite or prodrug thereof, wherein, R1, R2, R3, R4 and R5 are, for example, as defined in the specification. The compound can act as an ALK inhibitor, and is for preparing an anti-tumor medicament for suppressing an anaplastic lymphoma kinase.

2,4-dibasic miazines compound

The invention belongs to the field of medical chemistry, relates to a 2,4-dibasic miazines compound and specifically relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof, a drug compound thereof and an application thereof in treating EGFR or/and ALK mediated diseases.

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase

In the treatment of echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase positive (ALK+) non-small-cell lung cancer (NSCLC), secondary mutations within the ALK kinase domain have emerged as a major resistance mechanism to both first- and second-generation ALK inhibitors. This report describes the design and synthesis of a series of 2,4-diarylaminopyrimidine-based potent and selective ALK inhibitors culminating in identification of the investigational clinical candidate brigatinib. A unique structural feature of brigatinib is a phosphine oxide, an overlooked but novel hydrogen-bond acceptor that drives potency and selectivity in addition to favorable ADME properties. Brigatinib displayed low nanomolar IC50s against native ALK and all tested clinically relevant ALK mutants in both enzyme-based biochemical and cell-based viability assays and demonstrated efficacy in multiple ALK+ xenografts in mice, including Karpas-299 (anaplastic large-cell lymphomas [ALCL]) and H3122 (NSCLC). Brigatinib represents the most clinically advanced phosphine oxide-containing drug candidate to date and is currently being evaluated in a global phase 2 registration trial.

Nitric oxide donating anilinopyrimidines: Synthesis and biological evaluation as EGFR inhibitors

To search for potent nitric oxide (NO) donating epidermal growth factor receptor (EGFR) inhibitors, a series of phenylsulfonylfuroxan-based anilinopyrimidines 10a-h were synthesized and biologically evaluated. Compounds 10f-h exhibited potent inhibitory activity against EGFR L858R/T790M and were as potent as WZ4002 in inhibition of H1975 cells harboring EGFR L858R/T790M. Additionally, 10h produced high levels of NO in H1975 cells but not in normal human cells, and its antiproliferative activity was diminished by hemoglobin, an NO scavenger. Furthermore, 10h inhibited EGFR activation and downstream signaling in H1975 cells. These results suggest that the strong antiproliferative activity of 10h could be attributed to the synergic effects of high levels of NO production and inhibition of EGFR and downstream signaling in the cancer cells.

CHEMICAL COMPOUNDS

The present invention relates to compounds of Formula (I) and/or Formula (Ia): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the tr

COMPOUNDS AND THERAPEUTIC USES THEREOF

The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.

2- [ (2-{PHENYLAMINO}-1H-PYRROLO [2, 3-D] PYRIMIDIN-4-YL) AMINO] BENZAMIDE DERIVATIVES AS IGF-1R INHIBITORS FOR THE TREATMENT OF CANCER

Novel pyrrolopyrimidines as shown in formula (I) and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.

Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)

The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimi

Imidazopyridine Kinase Inhibitors

The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.