87753-08-0

Upstream product

• 39242-56-3 7a-morpholin-4-yl-2-phenyl-5,6,7,7a-tetrahydro-4aH-cyclopenta[e][1,3]oxazin-4-one 
• 936-52-7 1-(N-morpholino)cyclopent-1-ene 
• 4461-33-0 benzoyl isocyanate 
• 1506-75-8 2-bromo-1-cyclopentene-1-carboxylic acid 
• 1670-14-0 benzamidine monohydrochloride 
• 611-10-9 2-ethoxycarbonyl-1-cyclopentanone 
• 10472-24-9 methyl 2-oxocyclopentane-1-carboxylate 

Downstream Products

• 1436866-24-8 (2-phenyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl) trifluoromethanesulfonate 
• 1436866-26-0 2-[4-[(2-phenyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)amino]phenyl]acetic acid 
• 1436866-25-9 ethyl 2-[4-[(2-phenyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)amino]phenyl]acetate 

Relevant academic research and scientific papers

Synthesis and biological evaluation of novel 6,7-dihydro-5H-cyclopenta[d]pyrimidine and 5,6,7,8-tetrahydroquinazoline derivatives as sigma-1 (σ1) receptor antagonists for the treatment of pain

The synthesis and biological evaluation of new series of 6,7-dihydro-5H-cyclopenta[d]pyrimidine and 5,6,7,8-tetrahydroquinazoline derivatives as selective sigma-1 receptor (σ1R) antagonists are reported. The receptor affinities of new compounds

Synthesis and biological evaluation of novel sigma-1 receptor antagonists based on pyrimidine scaffold as agents for treating neuropathic pain

The discovery and synthesis of a new series of pyrimidines as potent sigma-1 receptor (σ1R) antagonists, associated with pharmacological antineuropathic pain activity, are the focus of this article. The new compounds were evaluated in vitro in σ-1 and σ-2 receptor binding assays. The nature of the pyrimidine scaffold was crucial for activity, and a basic amine was shown to be necessary according to the known pharmacophoric model. The most promising derivative was 5-chloro-2-(4-chlorophenyl)-4-methyl-6-(3-(piperidin-1-yl)propoxy)pyrimidine (137), which exhibited a high binding affinity to σ1R receptor (Ki σ1 = 1.06 nM) and good σ-1/2 selectivity (1344-fold). In in vivo tests, compound 137 exerted dose-dependent antinociceptive effects in mice formalin model and rats CCI models of neuropathic pain. In addition, no motor impairments were found in rotarod tests; acceptable pharmacokinetic properties were also noted. These data suggest compound 137 may constitute a novel class of drugs for the treatment of neuropathic pain.

Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors

2-Phenyl-4-piperidinyl-6,7-dihydrothieno[3,4-d]pyrimidine derivative (2) was found to be a new PDE4 inhibitor with moderate PDE4B activity (IC 50 = 150 nM). A number of derivatives with a variety of 4-amino substituents and fused bicyclic pyrim

Microwave-assisted copper-powder-catalyzed synthesis of pyrimidinones from β-bromo α,β-unsaturated carboxylic acids and amidines

β-Bromo α,β-unsaturated carboxylic acids were coupled and cyclized with amidine hydrochlorides by microwave irradiation in the presence of catalytic amounts of copper powder and a base to give the corresponding pyrimidinones in high yields. Georg Thieme Verlag Stuttgart New York.

Pyrimidine derivatives useful in the treatment of insulin resistance and hyperglycemia

This invention provides compounds of Formula I having the structure: wherein: B is alkyl of 1-4 carbons or alkoxy of 1-4 carbons; R1 is aryl or Het optionally substituted with R6; R2 and R3 are each independentl

A Novel Ring Transformation of Oxazinones and Azetidinones into Pyrimidinones

Azetidinones or oxazinones, being easily prepared from enamines and acyl isocyanates, were transformed into highly substituted 4(3H)-pyrimidinones upon treatment with ammonium acetate.This novel ring transformation was also accomplished through a one-pot