1227807-75-1

Basic information

• Product Name: C₁₁H₆ClFN₂O₂
• Synonyms: C₁₁H₆ClFN₂O₂
• CAS NO: 1227807-75-1
• Molecular Weight: 252.632
• Mol File: 1227807-75-1.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: C₁₁H₆ClFN₂O₂(CAS DataBase Reference)
• NIST Chemistry Reference: C₁₁H₆ClFN₂O₂(1227807-75-1)
• EPA Substance Registry System: C₁₁H₆ClFN₂O₂(1227807-75-1)

Safety Data

• Hazardous Substances Data: 1227807-75-1(Hazardous Substances Data)

Upstream product

• 913835-32-2 3-carboxy-4-chlorophenylboronic acid 
• 62802-42-0 2-chloro-5-fluoropyrimidine 

Downstream Products

• 1227808-80-1 C₁₈H₁₉ClFN₃O₂ 
• 1227808-86-7 C₁₉H₂₀ClF₂N₃O₂ 
• 1227808-89-0 C₁₉H₁₉ClF₃N₃O₂ 
• 1227808-92-5 C₁₈H₁₇ClF₃N₃O₂ 
• 1227808-95-8 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)-methyl)-5-(5-fluoropyrimidin-2-yl)benzamide 
• 1227808-83-4 C₁₇H₁₇ClFN₃O₂ 
• 1227808-77-6 C₁₉H₂₁ClFN₃O₂ 

Relevant articles and documents

2-CHLORO-N-[2-(1,3-THIAZOL-5-YL)ETHYL]-5-(5-FLUOROPYRIMIDIN-2-YL)-BENZAMIDES AND THEIR USE AS P2X7 RECEPTOR ANTAGONISTS

The present invention relates to novel substituted piperidine and morpholine compounds of formula (I) wherein X is O or CF2; R1 and R2 are independently selected from the group consisting of hydrogen, CH2OH, CH2F, CHF2, cyclopropyl, or -C≡CH with the proviso that when one of R1 and R2 is CH2OH, CH2F, CHF2, cyclopropyl or -C≡CH, then the other of R1 or R2 is hydrogen, having P2X7 receptor (P2X7) antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.

Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist

Focused SAR studies were carried out around 5-heteroaryl and 1-amide portions of the 2-chlorobenzamide scaffold, resulting in the discovery of a potent, metabolically stable and centrally penetrable antagonist against P2X7 receptor.