3-(Cyclopropylmethoxy)-4-(difluoromethoxy)benzoic acid

Synonym
Product Category
Product Code
CAS Number
MDL Number
Pubchem CID
Reaxys RN
3-Cyclopropylmethoxy-4-difluoromethoxybenzoic acid
Difluoromethylating Building Blocks, API & Intermediates
KUMI2F88
162401-62-9
MFCD04621687
2394006
11413145
image-155171-Trimethyl(trifluoromethyl)silane_reagent.png
Chemical Name
Molecular Formula
Molecular Weight
Assay
Appearance
Melting Point
Packaging
Storage
3-(Cyclopropylmethoxy)-4-(difluoromethoxy)benzoic acid
C12H12F2O4
258.22
≥98.0%
White Solid
118-120°C
5g,10g,25g,50g,100g,200g and 500g
Store at room temperature
3-(Cyclopropylmethoxy)-4-(difluoromethoxy)benzoic acid is a difluoromethylated building block and intermediate typically for the synthesis of Roflumilast, a selective and long-acting inhibitor of phosphodiesterase type 4 (PDE 4) for  the treatment of inflammatory conditions of the lungs such as chronic obstructive pulmonary disease(COPD).
A New Route to Roflumilast via Copper-Catalyzed Hydroxylation. [1]
A convenient method for the synthesis of roflumilast. [2]
Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases. [3]
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure–activity relationships. [4]
Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings. [5]
Discovery of N-Alkyl Catecholamides as Selective Phosphodiesterase-4 Inhibitors with Anti-neuroinflammation Potential Exhibiting Antidepressant-like Effects at Non-emetic Doses. [6]
References:
[1] F.Ni, et al, Synthesis(Germany), 2012, 44(23), pp 3598-3602.
[2] Y.Lin, et al, Res. Chem. Intermed., 2013, 39(5), pp 2107-2113.
[3] E.Armani, et al, J. Med. Chem., 2014, 75(3), pp 793-816.
[4] Z.Zhou, et al, Bioorg. Med. Chem., 2015, 23(22), pp 7332-7339.
[5] Z.Z.Zhou, et al, Eur. J. Med. Chem., 2016, 124, pp 372-379.
[6] Z.Z.Zhou, et al, ACS Chem. Neurosci., 2017, 8(1), pp 135-146.
Signal Word
Hazard Statements
Precautionary Statements
HS Code
RIDADR
Legal Information
Warning
H226,H302+H312+H332,H315,H319,H335
P210,P260,P271,P280
2918999090
NONH for all modes of transport

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