M.W=300-350 Archives - Amides-buliding-blocks

Iqbal, Saqib A.’s team published research in Angewandte Chemie, International Edition in 58 | CAS: 2246585-66-8

Angewandte Chemie, International Edition published new progress about 2246585-66-8. 2246585-66-8 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester, name is N-(4-Methyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)pivalamide, and the molecular formula is C18H28BNO3, Recommanded Product: N-(4-Methyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)pivalamide.

Iqbal, Saqib A. published the artcileAcyl-Directed ortho-Borylation of Anilines and C7 Borylation of Indoles using just BBr₃, Recommanded Product: N-(4-Methyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)pivalamide, the publication is Angewandte Chemie, International Edition (2019), 58(43), 15381-15385, database is CAplus and MEDLINE.

Indoles are privileged heterocycles found in many biol. active pharmaceuticals and natural products. However, the selective functionalization of the benzenoid moiety in indoles in preference to the more reactive pyrrolic unit is a significant challenge. Herein we report that N-acyl directing groups enable the C7-selective C-H borylation of indoles using just BBr₃. This transformation shows some functional-group tolerance and notably proceeds with C6 substituted indoles. The directing group can be readily removed in situ and the products isolated as the pinacol boronate esters. Acyl-directed electrophilic borylation can be extended to carbazoles and anilines with excellent ortho selectivity. 4-Amino-indoles are amenable to this process, with acyl group installation and directed electrophilic C-H borylation enabling selective formation of C5-BPin-indoles.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Iqbal, Saqib A.’s team published research in Angewandte Chemie, International Edition in 58 | CAS: 2246585-66-8

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Mashelkar, Karishma K.’s team published research in Pharmaceuticals in 14 | CAS: 1256359-16-6

Pharmaceuticals published new progress about 1256359-16-6. 1256359-16-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Sulfamide,Amine,Benzene,Boronic Acids,Boronate Esters, name is N-(4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)ethanesulfonamide, and the molecular formula is C14H22BNO4S, HPLC of Formula: 1256359-16-6.

Mashelkar, Karishma K. published the artcileDiscovery of a Novel Template, 7-Substituted 7-Deaza-4′-Thioadenosine Derivatives as Multi-Kinase Inhibitors, HPLC of Formula: 1256359-16-6, the publication is Pharmaceuticals (2021), 14(12), 1290, database is CAplus and MEDLINE.

The development of anticancer drugs remains challenging owing to the potential for drug resistance. The simultaneous inhibition of multiple targets involved in cancer could overcome resistance, and these agents would exhibit higher potency than single-target inhibitors. Protein kinases represent a promising target for the development of anticancer agents. As most multi-kinase inhibitors are heterocycles occupying only the hinge and hydrophobic region in the ATP binding site, we aimed to design multi-kinase inhibitors that would occupy the ribose pocket, along with the hinge and hydrophobic region, based on ATP-kinase interactions. Herein, we report the discovery of a novel 4′-thionucleoside template as a multi-kinase inhibitor with potent anticancer activity. The in vitro evaluation revealed a lead 1g (7-acetylene-7-deaza-4′-thioadenosine) with potent anticancer activity, and marked inhibition of TRKA, CK1δ, and DYRK1A/1B kinases in the kinome scan assay. We believe that these findings will pave the way for developing anticancer drugs.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics