55700-10-2Relevant articles and documents
Direct Oxidative Arylation of C(sp3)-H Bonds Adjacent to Oxygen of Ethers and Alcohols
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Paragraph 0022; 0079; 0095; 0096, (2017/04/26)
The present invention relates to a method for arylating ethers or alcohols through a C(sp^3)-H bond activity. More specifically, according to the method of the present invention, phenol which does not have a functional group such as -B(OH)_2 in ethers or alcohols reacts under a transition metal catalyst, so a novel-type sp^3C-H bond can be synthesized. The method does not have separately introduce a -B(OH)_2 functional group to a benzene ring. Phenol derivatives or naphthalene derivatives which can be commercially purchased react, so ethers or alcohols can be directly connected with a benzene ring including an OH group.COPYRIGHT KIPO 2017
Synthesis of 2-[(4-[18F]Fluorobenzoyloxy)methyl]-1,4- naphthalenedione from 2-hydroxymethyl 1,4-naphthoquinone and 4-[ 18F]fluorobenzoic acid using dicyclohexyl carbodiimide
Ackermann, Uwe,Sigmund, Duanne,Yeoh, Shinn Dee,Rigopoulos, Angela,O'Keefe, Graeme,Cartwright, Glenn,White, Jonathan,Scott, Andrew M.,Tochon-Danguy, Henri J.
, p. 788 - 794 (2012/05/20)
2-[(4-[18F]Fluorobenzoyloxy)methyl]-1,4-naphthalenedione ([ 18F]1) was synthesised as a putative hypoxia imaging agent from 2-hydroxymethyl 1,4-naphthoquinone (7) and 4-[18F]fluorobenzoic acid ([18F]8) using dicyclohexyl carbodiimide (DCC) to activate [ 18F]8. This coupling reaction was fast and gave quantitative yields. Further investigations are warranted on the use of DCC as a coupling agent in Positron Emission Tomography. The synthesis including HPLC purification and reformulation has been fully automated on a modified FDG synthesiser with two reactor vials. [18F]1 was produced in a radiochemical yield of 27 ± 5%, with a radiochemical purity of 97.5% and a specific activity of 78.4-134.5 GBq/μmol at the end of synthesis (n = 23). The total synthesis time including reformulation was 65 min. [18F]1 was found to be stable in plasma and saline, but underwent rapid metabolism in a phase 1 metabolite assay using rat S9 liver fractions. An in vivo evaluation of [ 18F]1 in transplanted, hypoxic SK-RC-52 tumour-bearing BALB/c nude mice revealed the tumour-to-muscle ratio to be 2.4 ± 0.1 at 2 h post-injection.
Synthesis of quinones from hydroquinone dimethyl ethers. Oxidative demethylation with cobalt(III) fluoride
Tomatsu, Ayumi,Takemura, Syunji,Hashimoto, Kimiko,Nakata, Masaya
, p. 1474 - 1476 (2007/10/03)
The oxidative demethylation of 1,4-dimethoxynaphthalene and 1,4- dimethoxybenzene derivatives with cobalt(III) fluoride proceeded in good to excellent yield to afford the corresponding naphthoquinone and benzoquinone derivatives.
