- Pd-Catalyzed Site-Selective p-Hydroxyphenyloxylation of Benzylic α-C(sp3)-H Bonds with 1,4-Benzoquinone
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A Pd-catalyzed, site-selective p-hydroxyphenyloxylation of benzylic α-C(sp3)-H bonds with 1,4-benzoquinone using thioamide as a directing group is reported. 1,4-Benzoquinone is employed as the p-hydroxyphenyloxy source without extra oxidants. T
- Song, Guangjun,Zheng, Ziwei,Wang, Yanhui,Yu, Xinhong
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supporting information
p. 6002 - 6005
(2016/12/09)
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- Copper-catalyzed amidation of acids using formamides as the amine source
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Copper-catalyzed amidation of acids with formamides or acetamide for the selective synthesis of amides with the aid of 1,4-diazabicyclo[2.2.2]octane as the ligand and tert-butyl hydroperoxide as the oxidant is presented. This method is highly compatible with a wide range of acids, including alkyl acids, aryl acids, α,β-unsaturated acids, and amino acids. A general and direct route for the synthesis of amides is described. The reaction involves the copper-catalyzed amidation of acids, wherein various formamides and an acetamide are used as the amine source. Importantly, this method represents a new strategy for the direct use of acids in the synthesis of amides. DABCO = 1,4-diazabicyclo[2.2.2]octane, TBHP = tert-butyl hydroperoxide. Copyright
- Xie, Ye-Xiang,Song, Ren-Jie,Yang, Xu-Heng,Xiang, Jian-Nan,Li, Jin-Heng
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p. 5737 - 5742
(2013/09/12)
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- 2-Phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives: Synthesis and antidepressant activity
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A series of 2-phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives was examined for the ability to inhibit both rat brain imipramine receptor binding and the synaptosomal uptake of norepinephrine (NE) and serotonin (5-HT). Neurotransmitter uptake inhibition was highest for a subset of 2-phenyl-2-(1-hydroxycyclohexyl)dimethylethylamines in which the aryl ring has a halogen or methoxy substituent at the 3- and/or 4-positions. Potential antidepressant activity in this subset was assayed in three rodent models - the antagonism of reserpine-induced hypothermia, the antagonism of histamine-induced ACTH release, and the ability to reduce noradrenergic responsiveness in the rat pineal gland. An acute effect seen in the rat pineal gland with several analogues, including 1-[1-(3,4-dichlorophenyl)-2-(dimethylamino)ethyl]cyclohexanol (23) and 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol (4), was taken as a possible correlate of a rapid onset of antidepressant activity. Compound 4 (venlafaxine) is presently undergoing clinical evaluation.
- Yardley,Morris Husbands,Stack,Butch,Bicksler,Moyer,Muth,Andree,Fletcher III,James,Sielecki
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p. 2899 - 2905
(2007/10/02)
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