- Radical scavengers: A practical solution to the reproducibility issue in the fluoridation of diaryliodonium salts
-
The addition of radical scavengers to the fluoridation of diaryliodonium salts was demonstrated to improve significantly both the reproducibility of the process and the material yield of the desired fluoroarene products. It was also established that the selectivity of the process was not influenced by the presence of the radical scavengers. TEMPO and galvinoxyl were found to be the most suitable radical scavengers in the fluoridation process allowing the methodology to be used routinely for the first time.
- Carroll, Michael A.,Nairne, James,Smith, Graham,Widdowson, David A.
-
-
Read Online
- Preparation method of 5-halo-2-alkyloxy-4-toluene sulfochloride
-
The invention relates to the technical field of chemical material intermediate synthesis, in particular to a preparation method of 5-halo-2-alkyloxy-4-toluene sulfochloride. The 5-halo-2-alkyloxy-4-toluene sulfochloride is formed by taking cheap and avail
- -
-
Paragraph 0043-0045
(2017/08/29)
-
- Efficient synthesis of aryl fluorides
-
Chemical Equation Presented Creating C-F bonds: A novel electrophilic fluorination of aryl and heteroaryl Crignard reagents has been discovered and was used for the efficient synthesis of various aryl fluoride derivatives (see picture; THF = tetrahydrofuran).
- Anbarasan, Pazhamalai,Neumann, Helfried,Beller, Matthias
-
experimental part
p. 2219 - 2222
(2010/06/17)
-
- Steric Effects on Atropisomerism in Tetraarylporphyrins
-
The rate of aryl ring rotation in a series of 5,10,15,20-tetrakis(2-X-5-methoxyphenyl)porphyrins, where X = H, F, Cl, Br, and I, was studied by NMR spectroscopy and chromatography.Where X = Cl, Br, and I, the four atropisomers αβαβ, ααββ, αααβ, and αααα w
- Crossley, Maxwell J.,Field, Leslie D.,Forster, Adrienne J.,Harding, Margaret M.,Sternhell, Sever
-
p. 341 - 348
(2007/10/02)
-
- Ring-substituted 1,2-dialkylated 1,2-bis(hydroxyphenyl)ethanes. 2. Synthesis and estrogen receptor binding affinity of 4,4'-, 5,5'-, and 6,6'-disubstituted metahexestrols
-
The synthesis of symmetrically 4,4'-, 5,5'-, and 6,6'-disubstituted derivatives of the mammary tumor inhibiting antiestrogen metahexestrol [meso-3,4-bis(3-hydroxyphenyl)hexane] (1) are described [4,4'-disubstituents: F(2), Cl (3), Br (4), I (5), CH2N(CH3)2 (6), CH3 (7), CH2OCH3 (8), CH2OC2H5 (9), CH2OH (10), NO2 (11), NH2 (12), N(CH3)2 (13), COCH3 (14), and C2H5 (15); 5,5'-substituents: OH (16) and Cl (17); 6,6'-disubstituents: OH (18), F (19), Cl (20), and CH3 (21)]. The synthesis of 1-3, 16, and 19 was accomplished by reductive coupling of the propiophenones with TiCl4/Zn and subsequent hydrogenation of the cis-3,4-diphenylhex-3-enes. Compounds 17, 18, 20, and 21 were synthesized by coupling the 1-phenyl-1-propanols with TiCl3/LiAlH4 and separation of the meso diastereomers, while 4-15 were obtained by substitution of metahexestrol. The binding affinity of these compounds to the calf uterine estrogen receptor was measured relative to that of [3H]estradiol by a competitive binding assay. The test compounds showed relative binding affinity (RBA) values between 15 and 0.5% were evaluated in the mouse uterine weight test. They showed a similar (2 and 12), slightly increased (19 and 21), or strongly enhanced (7 and 20) estrogenicity compared to that of metahexestrol. Compounds 1, 2, 7, 12, and 21 exhibited antiestrogenic activity inhibiting the estrone-stimulated uterine growth (24 to 60% inhibition).
- Hartmann,Heindl,Schonenberger
-
p. 577 - 585
(2007/10/02)
-