Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging was written by Andres, Jose-Ignacio;De Angelis, Meri;Alcazar, Jesus;Iturrino, Laura;Langlois, Xavier;Dedeurwaerdere, Stefanie;Lenaerts, Ilse;Vanhoof, Greet;Celen, Sofie;Bormans, Guy. And the article was included in Journal of Medicinal Chemistry in 2011.Related Products of 63071-12-5 This article mentions the following:
We have recently reported the phosphodiesterase 10A (PDE10A) inhibitor 2-[4-[1-(2-[18F]fluoroethyl)-4-pyridin-4-yl-1H-pyrazol-3-yl]-phenoxymethyl]-quinoline (I) as a promising candidate for in vivo imaging using positron emission tomog. (PET). We now describe the synthesis and biol. evaluation of a series of related pyridinyl analogs II (R1 = FCH2CH2, FCH2CH2CH2, F3CCH2; R2 = 3,5-di-Me, 5-methoxy, 6-bromo, etc.) that exhibit high potency and selectivity as PDE10A inhibitors. The most interesting compounds were injected in rats to measure their levels of PDE10A occupancy through an in vivo occupancy assay. The 3,5-dimethylpyridine derivative II (R1 = FCH2CH2, R2 = 3,5-di-Me) and the 5-methoxypyridine derivative II (R1 = FCH2CH2, R2 = 5-methoxy) showed a comparable level of occupancy to that of I. Because these derivatives showed lower in vitro activity and are slightly less lipophilic than I, we hypothesized that they could behave as better PET imaging ligands. Compounds II (R1 = 18FCH2CH2, R2 = 3,5-dimethyl; R1 = 18FCH2CH2, R2 = 5-methoxy; R1 = FCH2CH2, R2 = 5-11CH3O) were radio synthesized and subjected to biodistribution studies in rats for a preliminary evaluation as candidate PET radioligands for in vivo imaging of PDE10A in the brain. In the experiment, the researchers used many compounds, for example, (6-Methoxypyridin-2-yl)methanol (cas: 63071-12-5Related Products of 63071-12-5).
(6-Methoxypyridin-2-yl)methanol (cas: 63071-12-5) belongs to ethers. Ethers are good solvents partly because they are not very reactive. Most ethers can be cleaved, however, by hydrobromic acid (HBr) to give alkyl bromides or by hydroiodic acid (HI) to give alkyl iodides. Ethers feature bent C閳ユ彊閳ユ弲 linkages. In dimethyl ether, the bond angle is 111鎺?and C閳ユ彊 distances are 141 pm. The barrier to rotation about the C閳ユ彊 bonds is low. The bonding of oxygen in ethers, alcohols, and water is similar. In the language of valence bond theory, the hybridization at oxygen is sp3.Related Products of 63071-12-5
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem