16081-85-9

Upstream product

• 55-22-1 pyridine-4-carboxylic acid 
• 64188-97-2 3-aminopyridine-4-carboxamide 
• 108-88-3 toluene 
• 100-47-0 benzonitrile 
• 13958-99-1 3-bromopyridine-4-carboxamide 
• 52763-21-0 ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride 
• 1670-14-0 benzamidine monohydrochloride 
• 62259-93-2 C₂₀H₁₉N₃O 
• 1461603-03-1 ethyl 3-[(phenylcarbonyl)amino]-4-pyridinecarboxylate 
• 14208-83-4 ethyl 3-aminopyridine-4-carboxylate 
• 98-88-4 benzoyl chloride 
• 13959-02-9 3-bromoisonicotinic acid 
• 618-39-3 benzamidin 
• 849776-96-1 C₂H₄O₂*C₁₃H₁₃N₃O 

Downstream Products

• 849777-02-2 C₁₃H₈ClN₃ 
• 849776-89-2 C₁₈H₁₃N₅ 

Relevant academic research and scientific papers

Synthesis of Quinazolin-4(3 H)-ones via the Reaction of 2-Halobenzamides with Nitriles

This paper describes a convenient method to synthesize quinazolin-4(3H)-ones from simple and readily available 2-halobenzamides and nitriles. The Lewis acid Cu-catalyzed nucleophilic addition of 2-halobenzamide to nitriles followed by SNAr reaction proceeds smoothly in the presence of tBuOK as a base to produce quinazolinone derivatives.

Synthesis of 2-aryl quinazolinones: Via iron-catalyzed cross-dehydrogenative coupling (CDC) between N-H and C-H bonds

Herein, we describe the direct synthesis of quinazolinones via cross-dehydrogenative coupling between methyl arenes and anthranilamides. The C-H functionalization of the benzylic sp3 carbon is achieved by di-t-butyl peroxide under air, and the subsequent amination-aerobic oxidation process completes the annulation process. Iron catalyzed the whole reaction process and various kinds of functional groups were tolerated under the reaction conditions, providing 31 examples of 2-aryl quinazolinones using methyl arene derivatives in yields of 57-95percent. The synthetic potential has been demonstrated by the additional synthesis of aryl-containing heterocycles. This journal is

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives

Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived from pyrido[3,4-d]pyrimidin-4(3H)-one. A number of exemplars such as compound 41 possess interesting activity profiles in KDM4C and KDM5C biochemical and target-specific, cellular mechanistic assays.

TANKYRASE INHIBITORS

The present invention relates to a compound of formula I wherein X is C(R6) or N, Y is C or N, and ring A, ring B, R1 and R2 have the meanings defined herein, provided that when ring B is carbocyclic, X is C(R6); or a pharmaceutically acceptable salt or solvate thereof. The compounds are tankyrase-1 and tankyrase-2 inhibitors and are useful in the treatment of a number of conditions, including cancer.

QUINAZOLINE DERIVATIVES AS MEDICAMENTS

Quinazoline derivatives have the formula (I) or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0-3; wherein R1 is independently OH, SH, NH2, OR, SR, NHR, halo or R-halide; wherein two adjacent R1 groups may be joined to form an aliphatic hetero cycle ring of 5-6 members; wherein R2 is independently R, halo, R-halide, OR-halide, NH2, CONH2 or CONHR; wherein R is optionally substituted C1-C12 alkyl, C1-C12 alkenyl, C1-C12 alkynyl, or aryl C1-C12 alkyl, containing 0-4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are =O, =N, or OH; and wherein R3 is H or CH3. Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGFβ activity.