- Decarboxylative Negishi Coupling of Redox-Active Aliphatic Esters by Cobalt Catalysis
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A cobalt-catalyzed decarboxylative Negishi coupling reaction of redox-active aliphatic esters with organozinc reagents was developed. The method enabled efficient alkyl–aryl, alkyl–alkenyl, and alkyl–alkynyl coupling reactions under mild reaction conditions with no external ligand or additive needed. The success of an in situ activation protocol and the facile synthesis of the drug molecule (±)-preclamol highlight the synthetic potential of this method. Mechanistic studies indicated that a radical mechanism is involved.
- Liu, Xu-Ge,Zhou, Chu-Jun,Lin,Han, Xiang-Lei,Zhang, Shang-Shi,Li, Qingjiang,Wang, Honggen
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supporting information
p. 13096 - 13100
(2018/09/21)
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- N-ARYL AND N-HETEROARYL PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
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Provided herein are certain substituted N-aryl and N-heteroaryl piperidine compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R 6 are as defined. The said novel compounds, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-β receptor(LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory disease and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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Page/Page column 128
(2018/04/27)
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- Analogues of the low-efficacy partial GABAA agonist 4-PIOL. Syntheses and in vitro pharmacological studies
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4-PIOL (3-hydroxy-5-(4-piperidyl)isoxazole) is a low-efficacy GABAA agonist showing a dominating GABAA antagonist profile.Three dihydro analogues of 4-PIOL were synthesized, including (RS)-3-hydroxy-5-(4-piperidyl)-2-isoxazoline (1).The synthesis of 1 was based on a regioselective 1,3-dipolar cyclo-addition reaction between 1-benzyloxycarbonyl-4-vinylpiperidine (7) and bromonitrile oxide, prepared in situ from dibromoformoxime.Furthermore, the spiro analogues of 1 3-hydroxy-1-oxa-2,8-diazaspirodec-2-ene (2) and (RS)-3-hydroxy-1-oxa-2,7-diazaspirodec-2-ene (3) were synthesized regiospecifically via cycloaddition of bromonitrile oxide to the N-benzyloxycarbonyl-protected forms of 4-methylenepiperidine (11) and 3-methylenepiperidine (15) respectively.In contrast to 4-PIOL, none of the new compounds 1-3 showed detectable effects on the binding of 3H-GABAA or the subunit-selective GABAA agonist, 3H-THIP, to GABAA receptor sites, and they did not significantly affect the muscimol-stimulated binding of 3H-diazepam to the benzodiazepine site of the GABAA receptor complex.
- Amici, M De,Froelund, B,Hjeds, H,Krogsgaard-Larsen, P
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p. 625 - 631
(2007/10/02)
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