191218-48-1

Upstream product

• 1072-98-6 5-chloro-2-pyridylamine 
• 1999-00-4 ethyl 3-(4'-fluorophenyl)-3-oxopropionate 
• 1679-18-1 4-Chlorophenylboronic acid 
• 22288-66-0 2H,3H,4H-pyrido[1,2-a]pyrimidine-2,4-dione 
• 124-38-9 carbon dioxide 
• 504-29-0 2-aminopyridine 
• 20026-96-4 ethyl 3-(4-chlorophenyl)propiolate 
• 201230-82-2 carbon monoxide 
• 99-91-2 para-chloroacetophenone 
• 2881-63-2 ethyl (4-chlorobenzoyl)acetate 

Relevant academic research and scientific papers

Method for synthesizing pyrimidinone compound under participation of CO2

The invention provides a method for synthesizing a pyrimidinone compound under the participation of CO2, the structural formula of the pyrimidinone compound is shown as a formula (I), and a reaction substrate is shown as a formula (II); wherein R1, R2 and

Transition-metal-free lactamization of C(sp3)-H bonds with CO2: Facile generation of pyrido[1,2-: A] pyrimidin-4-ones

A novel carbonylation of C(sp3)-H bonds in pyridylamines with one atmosphere of CO2 is reported to synthesize important pyrimidinones in good yields. This transition-metal-free and redox-neutral process features the use of a nontoxic

Silver-catalyzed highly efficient synthesis of pyrido[1,2-a]pyrimidin-4-ones from 2-aminopyridines and alkynoates

Pyrimidinone is one of the important nitrogen containing heterocycles due to their wide range of bioactivities. An efficient silver-catalyzed intermolecular cyclization of 2-aminopyridines with various alkynoates has been developed. 2-Substituted 4H-pyrido[1,2-a]pyrimidin-4-ones containing a wide range of functional groups are synthesized in the standard conditions. This transformation is conducted under convenient conditions and affords products in good yields.

Scaffold-hopping of bioactive flavonoids: Discovery of aryl-pyridopyrimidinones as potent anticancer agents that inhibit catalytic role of topoisomerase IIα

A strategy of scaffold-hopping of bioactive natural products, flavones and isoflavones, leading to target-based discovery of potent anticancer agents has been reported for the first time. Scaffold-hopped flavones, 2-aryl-4H-pyrido[1,2-a]pyrimidin-4-ones and the scaffold-hopped isoflavones, 3-aryl-pyrido[1,2-a]pyrimidin-4-ones were synthesized via Pd-catalyzed activation–arylation methods. Most of the compounds were found to exhibit pronounced human topoisomerase IIα (hTopoIIα) inhibitory activities and several compounds were found to be more potent than etoposide (a hTopoIIα-inhibiting anticancer drug). These classes of compounds were found to be hTopoIIα-selective catalytic inhibitors while not interfering with topoisomerase I and interacted with DNA plausibly in groove domain. Cytotoxicities against various cancer cells, low toxicity in normal cells, and apoptotic effects were observed. Interestingly, compared to parent flavones/isoflavones, their scaffold-hopped analogs bearing alike functionalities showed significant/enhanced hTopoIIα-inhibitory and cytotoxic properties, indicating the importance of a natural product-based scaffold-hopping strategy in the drug discovery.

Synthesis of 2-Arylpyridopyrimidinones, 6-Aryluracils, and Tri- and Tetrasubstituted Conjugated Alkenes via Pd-Catalyzed Enolic C-O Bond Activation-Arylation

A new and efficient approach for the synthesis of biologically important 2-aryl-4H-pyrido[1,2-a]pyrimidin-4-ones and 6-aryluracils via previously unknown Pd-catalyzed enolic C-OH activation-arylation of pyridopyrimidin-2,4-diones and barbituric acids, res

Pd-catalyzed carbonylative cycloamidation of ketoimines for the synthesis of pyrido[1,2-a]pyrimidin-4-ones

The Pd(ii)-catalyzed pyridine-directed carbonylative cycloamidation of ketoimines has provided an efficient protocol for assembly of pyrido[1,2-a]pyrimidin-4-ones. This journal is

Method for treating tumors using 2-aryl-naphthyridin-4-ones

The present invention provides compounds of Formula I: STR1 wherein A and R1 -R8 are defined herein. The compounds of Formula I inhibit the polymerization of tubulin and possess antimitotic activity. The compounds of Formula I may be useful for the treatment of psoriasis, gout, papiloma, warts, and a variety of tumors.

Antitumor agents. 174. 2',3',4',5,6,7-Substituted 2-phenyl-1,8- naphthyridin-4-ones: Their synthesis, cytotoxicity, and inhibition of tubulin polymerization

Two series of 2',3',4',5,6,7-substituted 2-phenyl-l,8-naphthyridin-4- ones and 2-phenylpyrido[1,2-a]pyrimidin-4-ones have been synthesized and evaluated as cytotoxic compounds and as inhibitors of tubulin polymerization. Most 2-phenyl-1,8-naphthyridin-4-ones showed potent cytotoxic and antitubulin activities, whereas 2-phenylpyrido[1,2-a]pyrimidin-4-ones showed no activity in either assay. In general, a good correlation was found between cytotoxicity and inhibition of tubulin polymerization in the 2-phenyl-1,8- naphthyridin-4-one series. The 2-phenyl-1,8-naphthyridin-4-ones (44-49) with a methoxy group at the 3'-position showed potent cytotoxicity against most tumor cell lines with GI50 values in the low micromolar to nanomolar concentration range in the National Cancer Institute's 60 human tumor cell line in vitro screen. Introduction of substituents (e.g. F, Cl, CH3, and OCH3) at the 4'-position led to compounds with reduced or little activity and substitution at the 2'-position resulted in inactive compounds. The effects of various A-ring substitutions on activity depend on the substitution in ring C. Compounds 44-50 were potent inhibitors of tubulin polymerization, with activity nearly comparable to that of the potent antimitotic natural products colchicine, podophyllotoxin, and combretastatin A-4. Compounds 44-49 also inhibited the binding of radiolabeled colchicine to tubulin, but the inhibition was less potent than that obtained with the natural products. Further investigation is underway to determine if substitution at the 3'-position and multisubstitutions in ring C will result in compounds with increased activity.