351002-16-9

Basic information

• Product Name: 4H-Pyrido[1,2-a]pyrimidin-4-one, 9-bromo-7-methyl-2-(4-morpholinyl)-
• Synonyms: 4H-Pyrido[1,2-a]pyrimidin-4-one, 9-bromo-7-methyl-2-(4-morpholinyl)-;9-bromo-7-methyl-2-morpholino-4H-pyrido[1,2-a]pyrimidin-4-one;9-Bromo-7-methyl-2-(4-morpholinyl)-4H-pyrido[1,2-a]pyrimidin-4-one
• CAS NO: 351002-16-9
• Molecular Formula: C₁₃H₁₄BrN₃O₂
• Molecular Weight: 324.17
• Product Categories: Drug Intermediates
• Mol File: 351002-16-9.mol
• Article Data: 7

Chemical Properties

• Boiling Point: 447.3 °C at 760 mmHg
• Flash Point: 224.3 °C
• Appearance: /
• Density: 1.63
• Storage Temp.: Sealed in dry,Room Temperature
• PKA: 1.30±0.70(Predicted)
• CAS DataBase Reference: 4H-Pyrido[1,2-a]pyrimidin-4-one, 9-bromo-7-methyl-2-(4-morpholinyl)-(CAS DataBase Reference)
• NIST Chemistry Reference: 4H-Pyrido[1,2-a]pyrimidin-4-one, 9-bromo-7-methyl-2-(4-morpholinyl)-(351002-16-9)
• EPA Substance Registry System: 4H-Pyrido[1,2-a]pyrimidin-4-one, 9-bromo-7-methyl-2-(4-morpholinyl)-(351002-16-9)

Safety Data

• Hazardous Substances Data: 351002-16-9(Hazardous Substances Data)

Usage

General Description

4H-Pyrido[1,2-a]pyrimidin-4-one, 9-bromo-7-methyl-2-(4-morpholinyl)- is a chemical compound with a complex ring structure containing bromine and methyl groups, as well as a morpholine ring. It is a heterocyclic compound that may have potential pharmacological activity due to its unique structure. The bromine and methyl groups can potentially influence the compound's reactivity and solubility, while the presence of a morpholine ring suggests potential interactions with biological systems. Further research and analysis are needed to fully understand the properties and potential applications of this compound.

Upstream product

• 110-91-8 morpholine 
• 663619-90-7 9-bromo-2-hydroxy-7-methyl-4H-pyrido[1,2-a]pyrimidin-4-one 
• 17282-00-7 3-bromo-5-methylpyridin-2-amine 
• 1173900-34-9 9-bromo-2-hydroxy-7-methyl-4H-pyrido[1,2-a]pyrimidin-4-one hydrochloride 
• 1603-41-4 (5-methyl-pyridin-2-yl)amine 

Downstream Products

• 768401-13-4 MCA₅₂ 
• 663619-89-4 7-methyl-2-(4-morpholinyl)-9-[1-(phenylamino)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one 
• 1308384-67-9 TGX-D₃ 
• 1308384-66-8 TGX-D₂ 
• 1308384-68-0 TGX-D₄ 
• 1308384-65-7 TGX-D₁ 
• 1307864-99-8 C₂₉H₃₉N₅O₄ 
• 1307865-00-4 NH₂-SL-TGX 
• 1307864-98-7 C₂₄H₂₈N₄O₄ 
• 1173900-35-0 9-(1-hydroxyethyl)-7-methyl-2-morpholino-4H-pyrido[1,2-a]pyrimidin-4-one 
• 1374310-69-6 C₂₉H₃₈N₄O₄ 
• 1374310-68-5 C₃₉H₅₈N₄O₄ 

Relevant articles and documents

Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: Synthesis, biological evaluation and molecular modelling

A novel series of TGX-221 analogues was prepared and tested for their potency against the p110α, p110β, and p110δ isoforms of the PI3K enzyme, and in two cellular assays. The biological results were interpreted in terms of a p110β comparative model, in order to account for their selectivity towards this isoform. A CH2NH type linker is proposed to allow binding into the specificity pocket proposed to accommodate the high p110β-selectivity of TGX-221, although there was limited steric tolerance for substituents on the pendant ring with the 2-position most favourable for substitution.

Prodrug strategy for PSMA-targeted delivery of TGX-221 to prostate cancer cells

TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit. Recent studies showed that TGX-221 has antiproliferative activity against PTEN-deficient tumor cell lines including prostate cancers. The objective of this study was to develop an encapsulation system for parenterally delivering TGX-221 to the target tissue through a prostate-specific membrane aptamer (PSMAa10) with little or no side effects. In this study, PEG-PCL micelles were formulated to encapsulate the drug, and a prodrug strategy was pursued to improve the stability of the carrier system. Fluorescence imaging studies demonstrated that the cellular uptake of both drug and nanoparticles was significantly improved by targeted micelles in a PSMA positive cell line. The area under the plasma concentration time curve of the micelle formulation in nude mice was 2.27-fold greater than that of the naked drug, and the drug clearance rate was 6.16-fold slower. These findings suggest a novel formulation approach for improving site-specific drug delivery of a molecular-targeted prostate cancer treatment.

Enantiomerically Pure (-) 2-[1-(7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-A]pyrimidin-9-yl)ethylamino]benzoic Acid, Its Use In Medical Therapy, And A Pharmaceutical Composition Comprising It - 026

The present invention relates to enantiomerically pure (?) 2-[1-(7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)ethylamino]benzoic acid or pharmaceutically acceptable salts thereof, it being in a solid state, its use in medical therapy,