1260543-99-4

Basic information

• Product Name: ethyl 2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate
• Synonyms: ethyl 2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate;Ethyl 2-(4-morpholino-6-oxo-1,6-dihydropyrimidin-2-yl)acetate;ethyl [4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate;Ethyl 2-(4-morpholino-6-oxo-1H-pyrimidin-2-yl)acetate
• CAS NO: 1260543-99-4
• Molecular Formula: C₁₂H₁₇N₃O₄
• Molecular Weight: 267.29
• Mol File: 1260543-99-4.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• CAS DataBase Reference: ethyl 2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate(CAS DataBase Reference)
• NIST Chemistry Reference: ethyl 2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate(1260543-99-4)
• EPA Substance Registry System: ethyl 2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate(1260543-99-4)

Safety Data

• Hazardous Substances Data: 1260543-99-4(Hazardous Substances Data)

Usage

General Description

Ethyl 2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate is a chemical compound with a complex molecular structure. It belongs to the class of acetate esters and contains a 2-oxo-1,6-dihydropyrimidine ring with an attached morpholin-4-yl substituent. ethyl 2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate is synthesized by the condensation reaction of ethyl acetate with 4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidine-2-carboxylic acid. It may have potential applications in the field of medicinal chemistry, particularly in the design and development of new pharmaceutical drugs. Further research is needed to fully understand the properties, uses, and potential hazards associated with this chemical.

Upstream product

• 110-91-8 morpholine 
• 34570-16-6 ethyl β-amino-β-ethoxyacrylate hydrochloride 
• 2318-25-4 ethyl 3-ethoxy-3-iminopropanoate hydrochloride 

Downstream Products

• 1260544-11-3 C₁₇H₂₀N₄O₄ 
• 1374772-38-9 2-[(1-methyl-4-phenyl-1H-benzimidazol-2-yl)methyl]-6-(morpholin-4-yl)pyrimidin-4(3H)-one 
• 1374772-39-0 2-[(1-methyl-7-phenyl-1H-benzimidazol-2-yl)methyl]-6-(morpholin-4-yl)pyrimidin-4(3H)-one 
• 1374772-41-4 2-[(1-methyl-6-phenyl-1H-benzimidazol-2-yl)methyl]-6-(morpholin-4-yl)pyrimidin-4(3H)-one 
• 1374772-48-1 6-(morpholin-4-yl)-2-[(4-phenyl-1,3-benzoxazol-2-yl)methyl]pyrimidin-4(3H)-one 
• 1374772-49-2 6-(morpholin-4-yl)-2-[(7-phenyl-1,3-benzoxazol-2-yl)methyl]pyrimidin-4(3H)-one 
• 1374772-54-9 2-[(5-fluoro-4-phenyl-1,3-benzoxazol-2-yl)methyl]-6-(morpholin-4-yl)pyrimidin-4(3H)-one 
• 1260583-42-3 2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]-N-phenylacetamide 
• 1260544-02-2 N-(2-hydroxyphenyl)-2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetamide 
• 1260544-09-9 N-(5-fluoro-2-hydroxyphenyl)-2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetamide 
• 1260544-17-9 N-(3-fluoro-2-hydroxyphenyl)-2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetamide 
• 1260585-01-0 N-(2-hydroxy-3-methylphenyl)-2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetamide 
• 1260612-13-2 2-{2-[(2S)-2-methyl-2,3-dihydro-1H-indol-1-yl]-2-oxoethyl}-6-(morpholin-4-yl)pyrimidin-4(3H)-one 
• 1383973-89-4 6-(morpholin-4-yl)-2-[2-oxo-2-(4-phenyl-2,3-dihydro-1H-indol-1-yl)ethyl]pyrimidin-4(3H)-one 

Relevant articles and documents

Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers

Compelling molecular biology publications have reported the implication of phosphoinositide kinase PI3Kβ in PTEN-deficient cell line growth and proliferation. These findings supported a scientific rationale for the development of PI3Kβ-specific inhibitors for the treatment of PTEN-deficient cancers. This paper describes the discovery of 2-[2-(2,3-dihydro-indol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one (7) and the optimization of this new series of active and selective pyrimidone indoline amide PI3Kβ inhibitors. 2-[2-(2-Methyl-2,3-dihydro-indol-1-yl)-2- oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one (28), identified following a carefully designed methyl scan, displayed improved physicochemical and in vitro pharmacokinetic properties. Structural biology efforts enabled the acquisition of the first X-ray cocrystal structure of p110β with the selective inhibitor compound 28 bound to the ATP site. The nonplanar binding mode described herein is consistent with observed structure-activity relationship for the series. Compound 28 demonstrated significant in vivo activity in a UACC-62 xenograft model in mice, warranting further preclinical investigation. Following successful development, compound 28 entered phase I/Ib clinical trial in patients with advanced cancer.

NOVEL PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS

The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.

NOVEL 1H-PYRIMIDIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS INHIBITORS OF AKT (PKB) PHOSPHORYLATION

The invention relates to the novel products of formula (I): in which Z represents —O—, —NH or Nalk; n represents 0 to 4; R1 represents Hal, hydroxyl, alkyl or alkoxy; the alkyl and alkoxy radicals being optionally substituted; R2 and R3 represent H, Hal or alkyl optionally substituted with one or more halogen atoms; R4 represents H; these products being in all the isomer forms and the salts, as medicaments, in particular as inhibitors of AKT(PKB) phosphorylation.