401605-31-0

Upstream product

• 21740-00-1 5-bromo-2-iodo-benzoic acid 
• 100-46-9 benzylamine 
• 293738-03-1 5-bromo-2-iodobenzoyl chloride 

Downstream Products

• 450401-12-4 3-benzyl-6-bromo-2-methylquinazolin-4(3H)-one 
• 1403659-64-2 3-benzyl-6-bromo-2-phenylquinazolin-4(3H)-one 
• 1616629-20-9 3-benzyl-6-bromo-2-(4-oxopentyl)quinazolin-4(3H)-one 

Relevant academic research and scientific papers

Synthesis of 2-(1,2,3-Triazolyl)benzamide Derivatives by a Copper(I)-Catalyzed Multicomponent Reaction

The copper-catalyzed multicomponent reaction of 2-iodobenzamides, NaN3, and terminal alkynes for the synthesis of 2-(1,2,3-triazolyl)benzamide derivatives was achieved in a one-step process over a short period of time under mild conditions. The transformation involved a C(aryl)–N bond formation process followed by an azide–alkyne cycloadditon reaction. The absence of external base was crucial for the preferred reaction pathway to occur.

INHIBITORS OF EGFR AND METHODS OF USE THEREOF

The application relates to a compound having Formula Ia or Ib: (Ia) or (Ib), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.

DEGRADERS OF EGFR AND METHODS OF USE THEREOF

The application relates to a compound having Formula X: (X), wherein: the Targeting Ligand is capable of binding to EGFR, including drug resistant forms of EGFR; the Linker is a group that covalently binds to the Targeting Ligand and the Degron; and the Degron is capable of binding to a ubiquitin ligase, such as an E3 ubiquitin ligase (e.g., cereblon), wherein the Targeting Ligand is of Formula Ia or Ib: (Ia) or (Ib), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.

DEGRADERS OF EGFR AND METHODS OF USE THEREOF

The application relates to a compound having Formula (X), wherein: the Targeting Ligand is capable of binding to EGFR, including drug resistant forms of EGFR; the Linker is a group that covalently binds to the Targeting Ligand and the Degron; and the Degron is capable of binding to a ubiquitin ligase, such as an E3 ubiquitin ligase (e.g., cereblon), wherein the Targeting Ligand is of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.

INHIBITORS OF EGFR AND METHODS OF USE THEREOF

The application relates to a compound having Formula Ia or Ib: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.

PHARMACEUTICAL COMBINATIONS OF EGFR INHIBITORS AND METHODS OF USE THEREOF

The application relates to a pharmaceutical combination of an allosteric EGFR inhibitor of Formula Ia or Ib: (Ia) or (Ib), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and an ATP-competitive EGFR inhibitor of Formula I': (I'), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the combination, and a method of treating or preventing a disease in which EGFR plays a role.

PHARMACEUTICAL COMBINATIONS OF EGFR INHIBITORS AND METHODS OF USE THEREOF

The application relates to a pharmaceutical combination of an allosteric EGFR inhibitor of Formula Ia or Ib: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and an ATP-competitive EGFR inhibitor of Formula I': or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the combination, and a method of treating or preventing a disease in which EGFR plays a role.

Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors

Allosteric kinase inhibitors represent a promising new therapeutic strategy for targeting kinases harboring oncogenic driver mutations in cancers. Here, we report the discovery, optimization, and structural characterization of allosteric mutant-selective EGFR inhibitors comprising a 5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one scaffold. Our structure-based medicinal chemistry effort yielded an inhibitor (3) of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with an IC50 of a?10 nM and high selectivity, as assessed by kinome profiling. Further efforts to develop allosteric dibenzodiazepinone inhibitors may serve as the basis for new therapeutic options for targeting drug-resistant EGFR mutations.

Syntheses of quinazolinones from 2-iodobenzamides and enaminones via copper-catalyzed domino reactions

N-Substituted 2-iodobenzamides and enaminones undergo cascade transformations to achieve quinazolinones via a copper-catalyzed Ullmann-type coupling, a Michael addition and a retro-Mannich reaction. A unique stereochemical feature of this domino process was that Z-enaminones reacted without external ligands, whereas E-enaminones required the assistance of ligands. This journal is