33458-27-4

Usage

Uses

Used in Pharmaceutical Industry:
5-Pyrimidinecarboxylic acid, 1,2,3,4-tetrahydro-2-oxo-, ethyl ester is used as a key intermediate in the synthesis of various pharmaceutical compounds. Its unique chemical structure allows for the development of new drugs with potential therapeutic applications.
Used in Agrochemical Industry:
In the agrochemical industry, 5-Pyrimidinecarboxylic acid, 1,2,3,4-tetrahydro-2-oxo-, ethyl ester serves as a crucial building block for the production of agrochemicals, such as pesticides and herbicides. Its versatility in organic synthesis enables the creation of effective and targeted agrochemicals for agricultural use.
Used in Organic Synthesis:
5-Pyrimidinecarboxylic acid, 1,2,3,4-tetrahydro-2-oxo-, ethyl ester is used as a versatile intermediate in organic synthesis for the production of a wide range of chemical compounds. Its unique structure and reactivity make it a valuable component in the synthesis of various organic molecules with diverse applications.

Upstream product

• 2974-30-3 (Z)-ethyl-2-(ethoxymethyl)-3-methoxyacrylate 
• 57-13-6 urea 
• 763-69-9 ethyl 3-ethoxypropionate 
• 1086272-71-0 Ethyl (2E)-2-(ethoxymethyl)-3-methoxyacrylate 
• 879008-23-8 (Z)-ethyl-2-(ethoxymethyl)-3-methoxyacrylate 

Downstream Products

• 110099-99-5 2-CHLOROPYRIMIDINE-5-CARBONYLCHLORIDE 
• 1753-50-0 2-chloropyrimidine-5-carbonitrile 
• 1213234-72-0 (5-{2-[1-(3,4,5-Trichlorobenzyl)-1H-1,2,3-triazol-4-yl]pyrimidin-5-yl}-2H-tetrazol-2-yl)acetic acid 
• 856595-94-3 2-chloropyrimindine-5-carboxaminde 
• 1213234-95-7 2-[1-(3,4,5-trichlorobenzyl)-1H-1,2,3-triazol-4-yl]pyrimidine-5-carbonitrile 
• 1213234-96-8 5-(2H-tetrazol-5-yl)-2-[1-(3,4,5-trichlorobenzyl)-1H-1,2,3-triazol-4-yl]pyrimidine 
• 1213234-97-9 ethyl (5-{2-[1-(3,4,5-trichlorobenzyl)-1H-1,2,3-triazol-4-yl]pyrimidin-5-yl}-2H-tetrazol-2-yl)acetate 
• 1552310-52-7 2-chloro-4-(((5-(ethoxycarbonyl)pyrimidin-2-yl)(methyl)amino)methyl)benzoic acid 
• 1552310-58-3 ethyl 2-(3-chloro-4-(4-chloro-3-(pyridin-2-yl)phenylcarbamoyl)phenyl sulfonamido)pyrimidine-5-carboxylate 
• 1552310-69-6 ethyl 2-(4-((3-chloro-4-(4-chloro-3-(pyridin-2-yl)phenylcarbamoyl)phenyl sulfonamido)methyl)piperidin-1-yl)pyrimidine-5-carboxylate 
• 95928-49-7 2-hydroxy-pyrimidine-5-carboxylic acid ethyl ester 
• 1235451-75-8 ethyl 2-(methyl((4-morpholino-2-(1H-pyrrol-3-yl)thieno[3,2-d]pyrimidin-6-yl)methyl)amino)pyrimidine-5-carboxylate 
• 1339928-25-4 CUDC-907 
• 875318-46-0 ethyl 2-(4-(hydroxymethyl)piperidin-1-yl )pyrimidine-5-carboxylate 

Relevant academic research and scientific papers

COMBINATION THERAPY WITH A PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY

The invention provides a method of treating cancer in a subject in need thereof, comprising administering to the subject: (a) a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or an acyl group; and (b) a PD-1 signaling inhibitor; wherein the compound of Formula I or pharmaceutically acceptable salt thereof and the PD-1 signaling inhibitor are administered in amounts which in combination are therapeutically effective. The invention further provides a pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, a PD-1 signaling inhibitor and a pharmaceutically acceptable carrier or excipient.

COMBINATION THERAPY WITH A PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY

The invention provides a method of treating cancer in a subject in need thereof, comprising administering to the subject: (a) a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or an acyl group; and (b) a BCL-2 inhibitor; wherein the compound of Formula I or pharmaceutically acceptable salt thereof and a BCL-2 inhibitor are administered in amounts which in combination are therapeutically effective. The invention further provides a pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, a BCL-2 inhibitor and a pharmaceutically acceptable carrier or excipient.

PURINYL-N-HYDROXYL PYRIMIDINE FORMAMIDE DERIVATIVES, PREPARATION METHOD THEREFOR AND USE THEREOF

The Invention relates to the field of chemical medicines, and particularly to a purinyl-N-hydroxyl pyrimidine formamide derivative, preparation methods and uses thereof. The Invention provides a purinyl-N-hydroxyl pyrimidine formamide derivative with a st

Design and synthesis of novel androgen receptor antagonists via molecular modeling

Several androgen receptor (AR) antagonists are clinically prescribed to treat prostate cancer. Unfortunately, many patients become resistant to the existing AR antagonists. To overcome this, a novel AR antagonist candidate called DIMN was discovered by our research group in 2013. In order to develop compounds with improved potency, we designed novel DIMN derivatives based on a docking study and substituted carbons with heteroatom moieties. Encouraging in vitro results for compounds 1b, 1c, 1e, 3c, and 4c proved that the new design was successful. Among the newly synthesized compounds, 1e exhibited the strongest inhibitory effect on LNCaP cell growth (IC50= 0.35 μM) and also acted as a competitive AR antagonist with selectivity over the estrogen receptor (ER) and the glucocorticoid receptor (GR). A docking study of compound 1e fully supported these biological results. Compound 1e is considered to be a novel, potent and AR-specific antagonist for treating prostate cancer. Thus, our study successfully applied molecular modeling and bioisosteric replacement for hit optimization. The methods here provide a guide for future development of drug candidates through structure-based drug discovery and chemical modifications.

Phosphoinositide 3-kinase inhibitor with a zinc binding moiety

The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH ZINC BINDING MOIETY

PROBLEM TO BE SOLVED: To provide phosphoinositide 3-kinase inhibitors with a zinc binding moiety. SOLUTION: There is provided a compound represented by formula (I) in the figure. (X is S, O or the like; Y is CH, N or the like; G1 is optionally substituted N or the like; R1 and R2 are each independently H or the like; C is a substituted heterocycle or the like; B is a linear alkyl or the like; Ra and Rb together with the nitrogen atom coupled to them are morpholino or the like; G2 is an indazole ring or the like; q, r and s are independently from 0 to 1, provided that at least one of them is 1; t is from 0 to 1; n is from 0 to 4; and p is from 0 to 2.) COPYRIGHT: (C)2016,JPOandINPIT

HEDGEHOG ANTAGONISTS HAVING ZINC BINDING MOIETIES

The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The com-pounds can be used in methods of treating proliferative dis-eases and disorders such as cancer

HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE

Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and tr

TREATMENT OF CANCERS HAVING K-RAS MUTATIONS

The present invention provides a method of treating a cancer associated with a K- ras mutation in a subject in need thereof. The method comprises the steps of (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) adminsiterign to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

Synthesis of 4-unsubstituted dihydropyrimidines. Nucleophilic substitution at position-2 of dihydropyrimidines

Synthesis of novel 4-unsubstituted dihydropyrimidines (DPs) was performed. Subsequently, a variety of 4-unsubstituted 1,4(3,4)-DPs with amino moieties at position-2 were obtained in excellent yields by activation of position-2 owing to regioselective alkoxycarbonylation at position-3 of the DP skeleton. 3-Oxo-2-phenyl-2,3,5,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrimidine was obtained using phenylhydrazine instead of amines. Individual tautomers of 1,4(3,4)-DP were observed in the 1H NMR spectra of one derivative depending on temperature and concentration. On the other hand, only 1,4-DP was found in the solid state by single-crystal X-ray crystallography.