92566-52-4

Upstream product

• 623-49-4 ethyl cyanoformate 
• 38430-03-4 N-phenylbenzimidoyl chloride 
• 5439-98-5 2-phenyl-2,3-dihydro-phthalazine-1,4-dione 
• 2216-94-6 phenylpropynoic acid ethyl ester 
• 93-98-1 N-phenyl benzoyl amide 

Downstream Products

• 92566-59-1 1-[(2-phenylquinazolin-4-yl)-carbonyl]-piperidine-3-methanol 
• 92979-88-9 2-methyl-1-[(2-phenylquinazolin-4-yl)-carbonyl]-piperidine 
• 92566-51-3 N,N-diethyl-2-phenylquinazoline-4-carboxamide 
• 92566-57-9 2,3,4,5,6,7-hexahydro-1-[(2-phenylquinazolin-4-yl)-carbonyl]-azepine 
• 92979-89-0 3-methyl-1-[(2-phenylquinazolin-4-yl)-carbonyl]-piperidine 
• 92566-53-5 1-[(2-phenylquinazolin-4-yl)-carbonyl]-pyrrolidine 
• 92566-55-7 4-[(2-phenylquinazolin-4-yl)-carbonyl]-morpholine 
• 92309-78-9 2-Phenyl-quinazoline-4-carbonyl chloride 
• 7672-01-7 2-phenylquinazoline-4-carboxylic acid 

Relevant academic research and scientific papers

Ru(II)-Catalyzed C-H Activation and Annulation Reaction via Carbon-Carbon Triple Bond Cleavage

An unprecedented Ru(II)-catalyzed C-H activation and annulation reaction, which proceeds via C-C triple bond cleavage, is reported. This reaction of 2-phenyldihydrophthalazinediones with alkynes, which works most efficiently in the presence of bidented ligand 1,3-bis(diphenylphosphino)propane, affords good yields of substituted quinazolines.

Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework

A novel class of potent and selective non-peptide neurokinin-3 (NK-3) receptor antagonists, featuring the 4-quinolinecarboxamide framework, has been designed based upon chemically diverse NK-1 receptor antagonists. The novel compounds 33-76, prompted by chemical modifications of the prototype 4, have been characterized by binding analysis using a membrane preparation of chinese hamster ovary (CHO) cells expressing the human neurokinin-3 receptors (hNK-3-CHO), and clear structure-activity relationships (SARs) have been established. From SARs, (R)-N-[α-(methoxycarbonyl)benzyl]-2- phenylquinoline-4-carboxamide (65, SB 218795, hNK-3-CHO binding K(i) = 13 nM) emerged as one of the most potent compounds of this novel class. Selectivity studies versus the other neurokinin receptors (hNK-2-CHO and hNK-1-CHO) revealed that 65 is about 90-fold selective for hNK-3 versus hNK-2 receptors (hNK-2-CHO binding K(i) = 1221 nM) and over 7000-fold selective versus hNK-1 receptors (hNK-1-CHO binding K(i) = >100 μM). In vitro functional studies in rabbit isolated iris sphincter muscle preparation demonstrated that 65 is a competitive antagonist of the contractile response induced by the potent and selective NK-3 receptor agonist senktide with a K(b) = 43 nM. Overall, the data indicate that 65 is a potent and selective hNK-3 receptor antagonist and a useful lead for further chemical optimization.