16154-62-4

Upstream product

• 109-01-3 1-methyl-piperazine 
• 99-54-7 3,4-dichloronitrobenzene 
• 350-30-1 3-chloro-4-fluoronitrobenzene 

Downstream Products

• 16154-72-6 3-chloro-4-(4-methylpiperazin-1-yl)benzenamine 

Relevant academic research and scientific papers

PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER

The invention provides compounds of the formula (1): or a salt or tautomer thereof wherein A, R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are inhibitors of Wee1 and/or PLK1 kinase and are envisaged to be useful in the treatment of cancers.

The synthesis and bioactivity of pyrrolo[2,3-d]pyrimidine derivatives as tyrosine kinase inhibitors for NSCLC cells with EGFR mutations

EGFR mutations are an ongoing challenge in the treatment of NSCLC, and demand continuous updating of EGFR TKI drug candidates. Pyrrolopyrimidines are one group of versatile scaffolds suitable for tailored drug development. However not many precedents of this type of pharmacophore have been investigated in the realm of third generation of covalent EGFR-TKIs. Herein, a series of pyrrolo[2,3-d]pyrimidine derivatives able to block mutant EGFR activity in a covalent manner were synthesized, through optimized Buchwald-Hartwig C–N cross coupling reactions. Their preliminary bioactivity and corresponding inhibitory mechanistic pathways were investigated at molecular and cellular levels. Several compounds exhibited increased biological activity and enhanced selectivity compared to the control compound. Notably, compound 12i selectively inhibits HCC827 cells harboring the EGFR activating mutation with up to 493-fold increased efficacy compared to in normal HBE cells. Augmented selectivity was also confirmed by kinase enzymatic assay, with the test compound selectively inhibiting the T790 M activating mutant EGFRs (IC50 values of 0.21 nM) with up to 104-fold potency compared to the wild-type EGFR (IC50 values of 22 nM). Theoretical simulations provide structural evidence of selective kinase inhibitory activity. Thus, this series of pyrrolo[2,3-d]pyrimidine derivatives could serve as a starting point for the development of new EGFR-TKIs.

WEE1 inhibitors as well as preparation and application thereof

The invention relates to WEE1 inhibitors as well as preparation and application thereof. The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, solvates, polymorphs or isomers thereof, and their use in the preparation of medicaments for the treatment of diseases associated with WEE1 activity.

BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS

Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I through IV.

POTENT DUAL BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS

Disclosed herein are compounds that are inhibitors of BRD4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BRD4 are also disclosed. In certain aspects, disclosed are compounds of Formula I-IV.

PYRAZOLYL-PYRIMIDINES AS KINASE INHIBITORS

Disclosed are compounds having the formula (I): wherein Z, n, R1, R1A, R3, R4, and R5 are as defined herein, and methods of making and using the same.

Cobalt-catalyzed C-N bond-forming reaction between chloronitrobenzenes and secondary amines

Cyclic secondary amines react with mono- or dichloronitrobenzene in the presence of a catalytic amount of cobalt(II) chloride. Phosphane ligands are beneficial for the reaction, although the bite-angle effect was not strong. The nitro-substituted tertiary amines formed are important as bioactive compounds and can also be intermediates for the synthesis of substituted anilines. This work represents the first cobalt-catalyzed approach to C-N bond-forming reactions involving aromatic chlorides and cyclic secondary amines. The reaction is ortho- and para-selective, with meta-substituted halides being unreactive in this procedure. The first cobalt-catalyzed C-N bond-forming reaction involving aromatic chlorides and cyclic secondary amines is described.The reaction is ortho- and para-selective; meta-substituted halides are unreactive. Copyright

N-(3,4-disubstituted phenyl) salicylamide derivatives

A compound represented by the following formula (I) or a salt thereof: wherein R1, R2, R3 and R4 represent hydrogen atom, a halogen atom, cyano group, nitro group, a C1-4 alkyl group, a halogenated C

Nucleophilic substitutions on 3-chloro-4-fluoronitrobenzene

Nucleophilic substitutions on 3-chloro-4-fluoronitrobenzene 5 with piperazines occur on the fluorine rather than on the chlorine atom as reported, to yield 3-chloro-4-piperazinylnitrobenzenes 8 and 9.

9-(P-phenylazoanilino)-7-methyl-1H-imidazo[4,5-f]quinolines

A series of 9-(substituted amino)imidazo[4,5-f]quinolines are effective anthelmintic agents; particularly in respect to the tapeworm Hymenolepis nana.