877676-50-1

Basic information

• Product Name: (R)-2-chloro-7-ethyl-8-isopropyl-5-methyl-7,8-dihydropteridin-6(5H)-one
• Synonyms: (R)-2-chloro-7-ethyl-8-isopropyl-5-methyl-7,8-dihydropteridin-6(5H)-one;(7R)-2-Chloro-7-ethyl-7,8-dihydro-5-methyl-8-(1-methylethyl)-6(5H)-pteridinone;2-Chloro-7-ethyl-8-isopropyl-5-Methyl-7,8-dihydro-5H-pteridin-6-one;6(5H)-Pteridinone, 2-chloro-7-ethyl-7,8-dihydro-5-Methyl-8-(1-Methylethyl)-, (7R)-;(R)-2-Chloro-7-ethyl-8-isopropyl-5-methyl-6-oxo-5,6,7,8-tetrahydropyrimido[4,5-b]pyrazine
• CAS NO: 877676-50-1
• Molecular Formula: C₁₂H₁₇ClN₄O
• Molecular Weight: 268.74
• Mol File: 877676-50-1.mol
• Article Data: 8

Chemical Properties

• Appearance: /
• Density: 1.205
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• CAS DataBase Reference: (R)-2-chloro-7-ethyl-8-isopropyl-5-methyl-7,8-dihydropteridin-6(5H)-one(CAS DataBase Reference)
• NIST Chemistry Reference: (R)-2-chloro-7-ethyl-8-isopropyl-5-methyl-7,8-dihydropteridin-6(5H)-one(877676-50-1)
• EPA Substance Registry System: (R)-2-chloro-7-ethyl-8-isopropyl-5-methyl-7,8-dihydropteridin-6(5H)-one(877676-50-1)

Safety Data

• Hazardous Substances Data: 877676-50-1(Hazardous Substances Data)

Usage

Uses

(R)-2-Chloro-7-ethyl-8-isopropyl-5-methyl-7,8-dihydropteridin-6(5H)-one is a compound that has been involved in the preparation of selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain.

Upstream product

• 946161-16-6 methyl (2R)-2-[(2-chloro-5-nitropyrimidin-4-yl)(propan-2-yl)amino]butanoate 
• 947667-22-3 Methyl (2R)-2-(isopropylamino) butanoate 
• 889877-77-4 (7R)-2-chloro-7-ethyl-8-(propan-2-yl)-7,8-dihydropteridin-6(5H)-one 
• 74-88-4 methyl iodide 
• 512-56-1 trimethyl phosphite 
• 80-48-8 methyl p-toluene sulfonate 
• 616-38-6 carbonic acid dimethyl ester 

Downstream Products

• 1313518-61-4 (R)-7-ethyl-8-isopropyl-5-methyl-2-(2-phenyl-1H-imidazol-1-yl)-7,8-dihydropteridin-6(5H)-one 
• 1313518-97-6 (R)-7-ethyl-8-isopropyl-5-methyl-2-(5-phenyl-1H-pyrazol-1-yl)-7,8-dihydropteridin-6(5H)-one 
• 1313518-99-8 (R)-7-ethyl-8-isopropyl-5-methyl-2-(5-phenyl-1H-1,2,4-triazol-1-yl)-7,8-dihydropteridin-6(5H)-one 
• 1313519-06-0 (R)-7-ethyl-8-isopropyl-5-methyl-2-(2-phenyl-4,5-dihydro-1H-imidazol-1-yl)-7,8-dihydropteridin-6(5H)-one 
• 1280665-36-2 N-[(trans)-4-[4-(Cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-7-[[(7R)-7-ethyl-8-isopropyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-2,3-dihydrobenzofuran-4-carboxamide 
• 1333493-13-2 BI2536 
• 755038-65-4 Volasertib 
• 1280665-47-5 N-[(cis)-4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-7-[[(7R)-7-ethyl-8-isopropyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-2,3-dihydrobenzofuran-4-carboxamide 
• 755038-65-4 N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide 

Relevant articles and documents

PTERIDINONE COMPOUNDS AND USES THEREOF

The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).

Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors

Polo-like kinase-2 (Plk-2) is a potential therapeutic target for Parkinson's disease and this Letter describes the SAR of a series of dihydropteridinone based Plk-2 inhibitors. By optimizing both the N-8 substituent and the biaryl region of the inhibitors we obtained single digit nanomolar compounds such as 37 with excellent selectivity for Plk-2 over Plk-1. When dosed orally in rats, compound 37 demonstrated a 41-45% reduction of pS129-α-synuclein levels in the cerebral cortex.

DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF

Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.