- Direct Access to Primary Amines from Alkenes by Selective Metal-Free Hydroamination
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Direct and selective synthesis of primary amines from easily available precursors is attractive yet challenging. Herein, we report the rapid synthesis of primary amines from alkenes via metal-free regioselective hydroamination at room temperature. Ammonium carbonate was used as ammonia surrogate for the first time, allowing for efficient conversion of terminal and internal alkenes into linear, α-branched, and α-tertiary primary amines under mild conditions. This method provides a straightforward and powerful approach to a wide spectrum of advanced, highly functionalized primary amines which are of particular interest in pharmaceutical chemistry and other areas.
- Du, Yi-Dan,Chen, Bi-Hong,Shu, Wei
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supporting information
p. 9875 - 9880
(2021/03/29)
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- N6-Substituted Adenosine Receptor Agonists: Potential AntihypertensiveAgents
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Adenosine is known to exert a wide range of pharmacological effects including hypotension.This effect of adenosine suggested that modified analogues of adenosine might provide useful antihypertensive agents.Thus, we prepared a series of novel N6/sup
- Trivedi, B. K.,Blankley, C. J.,Bristol, J. A.,Hamilton, H. W.,Patt, W. C.,et al.
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p. 1043 - 1049
(2007/10/02)
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- Serotonin Receptor Affinity of Cathinone and Related Analogues
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A series of cathinone (α-aminopropiophenone) analogues was examined using the isolated rat fundus preparation. (S)-(-)-Cathinone possesses twice the serotonin receptor affinity of (+/-)-cathinone and four times the affinity of racemic amphetamine.Several derivatives of cathinone were found to either possess a lower affinity than the parent compound or did not interact with the receptors in a competitive manner.Several novel analogues, 1-(aminomethyl)-3,4-dihydronaphthalene hydrochloride (3), 4-(aminomethyl)-3-chromene hydrochloride (4b), as well as its 6-methoxy derivative, 4a, interact with serotonin receptors but in a fashion which is, most likely, dissimilar to the interaction of the substituted cathinone analogues.
- Glennon, Richard A.,Liebowitz, Stephen M.
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p. 393 - 397
(2007/10/02)
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