75438-78-7

Basic information

• Product Name: 4,6-Dichloro-2-Cyclopropyl-5-Nitropyrimidine
• Synonyms: 4,6-Dichloro-2-Cyclopropyl-5-Nitropyrimidine
• CAS NO: 75438-78-7
• Molecular Formula: C7H5Cl2N3O2
• Molecular Weight: 234.0395
• Mol File: 75438-78-7.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 4,6-Dichloro-2-Cyclopropyl-5-Nitropyrimidine(CAS DataBase Reference)
• NIST Chemistry Reference: 4,6-Dichloro-2-Cyclopropyl-5-Nitropyrimidine(75438-78-7)
• EPA Substance Registry System: 4,6-Dichloro-2-Cyclopropyl-5-Nitropyrimidine(75438-78-7)

Safety Data

• Hazardous Substances Data: 75438-78-7(Hazardous Substances Data)

Upstream product

• 7024-58-0 2-cyclopropyl-4,6-dihydroxy-pyrimidine 
• 75438-77-6 2-cyclopropyl-4,6-dihydroxy-5-nitro-pyrimidine 

Downstream Products

• 1397686-43-9 C₁₆H₁₅N₉ 
• 1397685-81-2 C₂₀H₂₅N₇ 
• 1397685-72-1 C₁₄H₁₃ClN₆ 
• 1305115-67-6 3-{[(2R)-4-benzylmorpholin-2-yl]methyl}-5-cyclopropyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-amine 
• 1305117-31-0 3-{[(2R)-4-benzylmorpholin-2-yl]methyl}-7-chloro-5-cyclopropyl-3H-[1,2,3]triazolo[4,5-d]pyrimidine 
• 1305117-30-9 N₄-{[(2S)-4-benzylmorpholin-2-yl]methyl}-6-chloro-2-cyclopropylpyrimidine-4,5-diamine 

Relevant articles and documents

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PDE8B is a cAMP-specific isoform of the broader class of phosphodiesterases (PDEs). As no selective PDE8B inhibitors had been reported, a high throughput screen was run with the goal of identifying selective tools for exploring the potential therapeutic utility of PDE8B inhibition. Of the numerous hits, one was particularly attractive since it was amenable to rapid deconstruction leading to inhibitors with very high ligand efficiency (LE) and lipophilic ligand efficiency (LLE). These triazolopyrimidines were optimized for potency, selectivity and ADME properties ultimately leading to compound 42. This compound was highly potent and selective with good bioavailability and advanced into pre-clinical development.

SUBSTITUTED TRIAZOLOPYRIMIDINES AS PDE8 INHIBITORS

Compounds of Formula (I): wherein R1 , R2, R3, R4, and R5 are as defined herein, are disclosed.

First dual M3 antagonists-PDE4 inhibitors: Synthesis and SAR of 4,6-diaminopyrimidine derivatives

SAR around 4,6-diaminopyrimidine derivatives allowed the discovery of the first potent dual M3 antagonists and PDE4 inhibitors. Various chemical modulations around that scaffold led to the discovery of ucb-101333-3 which is characterized by the

CHEMICAL COMPOUNDS WITH DUAL ACTIVITY, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS

The present invention concerns chemical compounds combining affinity and antagonism against the human m3 muscarinic receptor with activity as selective phosphodiesterase IV (PDE IV) inhibitors, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.