1007206-27-0

Basic information

• Product Name: 4-(4,6-dichloro-5-(2-chloroethyl)pyriMidin-2-yl)Morpholine
• Synonyms: 4-(4,6-dichloro-5-(2-chloroethyl)pyriMidin-2-yl)Morpholine;1. 4-(4,6-dichloro-5-(2-chloroethyl)pyrimidin-2-yl)morpholine
• CAS NO: 1007206-27-0
• Molecular Formula: C₁₀H₁₂Cl₃N₃O
• Molecular Weight: 297
• Mol File: 1007206-27-0.mol

Chemical Properties

• Appearance: /
• Storage Temp.: 2-8°C
• CAS DataBase Reference: 4-(4,6-dichloro-5-(2-chloroethyl)pyriMidin-2-yl)Morpholine(CAS DataBase Reference)
• NIST Chemistry Reference: 4-(4,6-dichloro-5-(2-chloroethyl)pyriMidin-2-yl)Morpholine(1007206-27-0)
• EPA Substance Registry System: 4-(4,6-dichloro-5-(2-chloroethyl)pyriMidin-2-yl)Morpholine(1007206-27-0)

Safety Data

• Hazardous Substances Data: 1007206-27-0(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
4-(4,6-dichloro-5-(2-chloroethyl)pyrimidin-2-yl)Morpholine is used as a key intermediate in the synthesis of various pharmaceuticals for its potential biological activity. Its unique structure allows for the development of new drugs with specific therapeutic properties.
Used in Agrochemical Industry:
In the agrochemical sector, 4-(4,6-dichloro-5-(2-chloroethyl)pyrimidin-2-yl)Morpholine is utilized as a building block in the creation of novel agrochemicals, contributing to the development of effective pesticides and other agricultural products.
Used in Medicinal Chemistry Research:
4-(4,6-dichloro-5-(2-chloroethyl)pyrimidin-2-yl)Morpholine is employed as a research molecule in medicinal chemistry, where its structure and properties are investigated to understand its potential interactions with biological targets and its role in the development of new therapeutic agents.
Used in Drug Discovery:
4-(4,6-dichloro-5-(2-chloroethyl)pyriMidin-2-yl)Morpholine plays a crucial role in drug discovery research, where its unique features are explored for the identification of new lead compounds and the optimization of drug candidates with improved pharmacological properties.
Overall, 4-(4,6-dichloro-5-(2-chloroethyl)pyrimidin-2-yl)Morpholine's diverse applications across different industries highlight its importance as a versatile and promising chemical entity in the fields of pharmaceuticals, agrochemicals, and scientific research.

Upstream product

• 127915-15-5 2-oxotetrahydrofuran-3-carboxylic acid methyl ester 
• 5638-78-8 morpholinoformamidine hydrochloride 
• 157415-17-3 Morpholine-4-carboxamidine; hydrobromide 
• 1178564-17-4 5-(2-hydroxyethyl)-2-morpholin-4-yl-pyrimidine-4,6-diol 

Downstream Products

• 1007215-39-5 6-chloro-5-(2-chloroethyl)-N-[(4-methoxyphenyl)methyl]-2-morpholinopyrimidin-4-amine 
• 1178564-27-6 4-chloro-7-methanesulfonyl-2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine 
• 1007206-24-7 4-(4-chloro-7-(pyridin-3-yl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-2-yl)morpholine 
• 1007207-67-1 CH5132799 
• 1007208-63-0 [3-[4-[2-[bis[(4-methoxyphenyl)methyl]amino]pyrimidin-5-yl]-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]phenyl]-(4-methylpiperazin-1-yl)methanone 
• 1007208-13-0 4-[4-[2-[bis[(4-methoxyphenyl)methyl]amino]pyrimidin-5-yl]-2-morpholino-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]benzaldehyde 
• 1007209-85-9 5-[2-morpholino-7-[4-(morpholinomethyl)phenyl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amine 
• 1007208-40-3 [4-[4-(2-aminopyrimidin-5-yl)-2-morpholino-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]phenyl]-(4-methylpiperazin-1-yl)methanone 
• 1007210-13-0 [4-(4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl)-phenyl]-(4-methyl-piperazin-1-yl)-methanone 
• 1007208-67-4 5-(2-morpholino-7-phenyl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine 
• 1007207-65-9 N,N-bis[(4-methoxyphenyl)methyl]-5-(2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine 
• 1007208-62-9 [3-[4-(2-aminopyrimidin-5-yl)-2-morpholino-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]phenyl]-(4-methylpiperazin-1-yl)methanone 

Relevant articles and documents

BICYCLIC HETEROARENES AND METHODS OF THEIR USE

Disclosed are compounds useful in the treatment of neurological disorders. The compounds described herein, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological diseases.

Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability

Phosphoinositide 3-kinase (PI3K) is activated in various human cancer cells and well known as a cancer therapy target. We previously reported a dihydropyrrolopyrimidine derivative as a highly potent PI3K inhibitor that has strong tumor growth inhibition in a xenograft model. In this report, we describe further optimization to improve its bioavailability.

Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation

Our lead compound for a phosphoinositide 3-kinase (PI3K) inhibitor (1) was metabolically unstable because of rapid glucuronidation of the phenol moiety. Based on structure-activity relationship (SAR) information and a FlexSIS docking simulation score, aminopyrimidine was identified as a bioisostere of phenol. An X-ray structure study revealed a hydrogen bonding pattern of aminopyrimidine derivatives. Finally, aminopyrimidine derivatives 33 showed strong tumor growth inhibition against a KPL-4 breast cancer xenograft model in vivo.

Discovery and biological activity of a novel class i PI3K inhibitor, CH5132799

Phosphatidylinositol 3-kinase (PI3K) is a lipid kinase and a promising therapeutic target for cancer. Using structure-based drug design (SBDD), we have identified novel PI3K inhibitors with a dihydropyrrolopyrimidine skeleton. Metabolic stability of the first lead series was drastically improved by replacing phenol with aminopyrimidine moiety. CH5132799, a novel class I PI3K inhibitor, exhibited a strong inhibitory activity especially against PI3Kα (IC50 = 0.014 μM). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice.

PYRROLOPYRIMIDIN DERIVATIVE FOR USE AS PI3K INHIBITOR, AND USE THEREOF

A preventive or therapeutic agent of a proliferative disease such as cancer, having superior PI3K inhibitory effects, superior cell proliferation inhibitory action as well as superior stability in a body and water solubility, is provided. A compound represented by formula (I): [wherein, Q represents a linking group represented by -X-Y-; X represents a single bond -CO-, -CONH-, -CON(C1-4 alkyl)-, -CS-, -CSNH-, -CSN(C1-4 alkyl)-, or -SO2-; Y represents a single bond, arylene or heteroarylene; provided that X and Y are not simultaneously single bonds; and R1 represents -C0-6 alkylene-(A)m-C1-6 alkyl, or C0-6 alkylene-(A)m-C0-6 alkylene-(heterocycle)] or a pharmaceutically acceptable salt thereof.

PYRIMIDINE DERIVATIVE AS PI3K INHIBITOR AND USE THEREOF

A drug is provided that is useful as a preventive or therapeutic for cancer as a result of having superior PI3K inhibitory effects as well as superior stability in the body and water-solubility. A compound, or pharmaceutically acceptable salt thereof, rep