37439-78-4Relevant academic research and scientific papers
Silver-Mediated Trifluoromethoxylation of (Hetero)aryldiazonium Tetrafluoroborates
Yang, Yu-Ming,Yao, Jian-Fei,Yan, Wei,Luo, Zhuangzhu,Tang, Zhen-Yu
supporting information, p. 8003 - 8007 (2019/10/11)
Here we report a silver-mediated trifluoromethoxylation of (hetero)aryldiazonium tetrafluoroborates by converting an aromatic amino group into an OCF3 group. This method, which can be considered to be a trifluoromethoxylation variation of the classic Sandmeyer-type reaction, uses readily available aryl and heteroaromatic amines as starting materials and AgOCF3 as trifluoromethoxylating reagents. The broad substrate scope and simple, mild reaction condition made this transformation a valuable method in constructing aryl-OCF3 bonds.
Synthesis and anti-proliferative activity of substituted- anilinoquinazolines and its relation to EGFR inhibition
El Ella,Saleh,Hassan,Hamdy,El-Araby,Abouzid
, p. 360 - 366 (2012/10/29)
4-Anilinoquinazoline is a privileged scaffold in developing small molecule inhibitors of tyrosine kinases (TK) especially epidermal growth factor receptor (EGFR). 2 series belonging to 3'-substituted-4-anilinoquinazoline scaffold were synthesized and screened in vitro on isolated and a breast cancer cell line. The research aims at exploring the activity of compounds having diverse substituents at 3' position of the aniline moiety. Generally, the meta-substituted-anilinoquinazolines exhibited significant inhibitory activity against isolated enzyme as well as MCF-7 cancer cell line. For instance, compound 10b inhibited >99% of EGFR activities at 10 M concentration. 6 of the tested compounds exhibited range of anti-proliferative activity below 10 M potency. In particular, compounds 6e and 10b displayed the highest activity among the tested compounds with IC50 values equal to 8.6 and 4.84 M, respectively. Structure-based tools were utilized to rationalize EGFR-TK binding of compound 10b since it is the most active compound in the enzyme inhibition test. Georg Thieme Verlag KG Stuttgart.New York.
1-(PIPERIDIN-4-YL)-1H-INDOLE DERIVATIVE
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Page/Page column 34-35, (2010/11/28)
The present invention provides a compound represented by the formula (1) or a pharmacologically acceptable salt thereof, or a hydrate thereof (provided that a compound in which all of R4a, R4b, and R4c are hydrogen atoms is excluded.): [wherein R1 represents a hydrogen atom, R2 represents a hydrogen atom, R3 represents the formula: wherein R4a, R4b, and R4c are the same as or different from each other and each represents a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group, etc.]
Synthesis of 7-methoxybenzolactam-V8 using a diastereoselective Strecker synthesis
Sakamuri,Kozikowski
, p. 475 - 476 (2007/10/03)
7-Methoxybenzolactam-V8 (4) was synthesized using a diastereoselective Strecker reaction as the key step employing an ortho-substituted phenylacetaldehyde and (R)-phenylglycinol as the chiral auxiliary.
