1-(trifluoromethyl)cyclopropane-1-carboxylic acid

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CAS Number
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Reaxys RN
1-(trifluoromethyl)cyclopropanecarboxylic acid
Trifluoromethyl Building Blocks
Chemical Name
Molecular Formula
Molecular Weight
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Boiling Point
1-(trifluoromethyl)cyclopropane-1-carboxylic acid
White to Yellow Solid
1g,5g,10g,25g,50g,100g and 500g
Store at room temperature
1-(trifluoromethyl)cyclopropane-1-carboxylic acid is a useful trifluoromethylated azetidine building block for the synthesis of various pharmaceutical compounds, such as P38 kinase inhibitors,GPR119 agonists, inhibitors of Hepatitis C virus replication,TRP-M8 receptor ligands and dipeptidyl peptidase-IV inhibitors and VLA-4 integrin antagonists, etc..
Selective reactions of 1,1-cycloalkanedicarboxylic acids with SF4. a route to 1,1-bis(trifluoromethyl)cycloalkanes, 1-fluoroformyl-1-(trifluoromethyl) cycloalkanes and 1-(trifluoromethyl)-1-cycloalkanecarboxylic acids. [1]
New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells. [2]
Imidazopyridines: A novel class of hNav1.7 channel blockers. [3]
Imidazopyridines as VLA-4 integrin antagonists. [4]
Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity. [5]
Oxadiazole-diarylpyrazole 4-carboxamides as cannabinoid CB1 receptor ligands. [6]
Synthesis and structure-activity relationship of 1,2,4-triazole-containing diarylpyrazolyl carboxamide as CB1 cannabinoid receptor-ligand. [7]
Discovery of MK-5046, a potent, selective bombesin receptor subtype-3 agonist for the treatment of obesity. [8]
Optimization of pharmacokinetics through manipulation of physicochemical properties in a series of HCV inhibitors. [9]
Lead optimization of 4,4-biaryl piperidine amides as γ-secretase inhibitors. [10]
Simple sulfinate synthesis enables C-H trifluoromethylcyclopropanation. [11]
Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors. [12]
Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain. [13]
[1] W.Dmowski, et al, J. F. Chem., 2000, 102(1-2), pp 141-146.
[2] F.E.Nielsen, et al, J. Med. Chem., 2006, 49(14), pp 4127-4139.
[3] C.London, et al, Bioorg. Med. Chem. Lett., 2008, 18(5), pp 1696-1701.
[4] D.J.Phillips, et al, Bioorg. Med. Chem. Lett., 2008, 18(14), pp 4146-4149.
[5] S.H.Lee, et al, J. Med. Chem., 2008, 51(22), pp 7216-7233.
[6] S.H.Lee, et al, Bioorg. Med. Chem. Lett., 2009, 19(7), pp 1899-1902.
[7] H.J.Lee, et al, Bioorg. Med. Chem., 2010, 18(3), pp 1149-1162.
[8] I.K.Sebhat, et al, Med. Chem. Lett., 2011, 2(1), pp 43-47.
[9] S.E.Lazerwith, et al, Med. Chem. Lett., 2011, 2(10), pp 715-719.
[10] J.Close, et al, Bioorg. Med. Chem. Lett., 2012, 22(9), pp 3202-3207.
[11] R.Gianatassio, et al, Angew. Chem. Int. Ed. Engl., 2014, 53(37), pp 9851-9855.
[12] K.Nakajima, et al, Angew. Chem. Int. Ed. Engl., 2016, 26(4), pp 1245-1248.
[13] S.Han, et al, Med. Chem. Lett., 2017, 8(12), pp1309-1303.
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