19938-01-3Relevant academic research and scientific papers
Nickel-catalyzed reductive defluorination of iodo allylic: Gem -difluorides: Allenyl monofluoride synthesis
You, Yiming,Wu, Jiayue,Yang, Lixin,Wu, Tao
supporting information, p. 1970 - 1973 (2022/02/19)
As a potential fluorinated synthon, there have been only limited reports on fluorinated allene synthesis and applications due to concerns about their stability. Here, we developed a nickel-catalyzed reductive defluorination of iodo allyl gem-difluorides to afford allenyl monofluorides under mild conditions with good functional group tolerance, which were easily converted to other C-F bond compounds, such as alkyl and alkenyl fluorides. Preliminary mechanistic studies suggested that monofluoroallenes were yielded by β-F elimination of the alkenyl C-Ni intermediates from the oxidative addition of C-I bonds to a nickel(0) catalyst, while zinc regenerates the catalyst and closes the catalytic cycle.
PYRAZOLO-TETRAHYDROPYRIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 21, (2011/02/18)
The invention relates to novel pyrazolo-tetrahydropyridines compounds and their use as orexin receptor antagonists.
PYRAZOLO-TETRAHYDRO PYRIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 10; 17, (2009/04/24)
The invention relates to novel pyrazolo-tetrahydropyridines compounds and their use as orexin receptor antagonists.
5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES
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Page/Page column 53, (2008/12/06)
The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I),wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
SUBSTITUTED PROPIONYL DERIVATIVES
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, (2008/06/13)
The present invention relates to a compound represented by the following formula (1): [wherein, X1represents a carboxyl group which may be esterified or the like group; Y1represents a single bond, -O- or -N(R1)-; at least one of A1, A2and A3is a group represented by the following formula (2): -R2-a1-R3-a2→{wherein, R2represents a divalent C2-12hydrocarbon group, R3represents a single bond or a divalent C1-12hydrocarbon group, a1and a2individually represent a single bond, -S-, -SO-, -SO2-, -SO2NH-, -O-, -N(R4)-, -CON(R5)-, -C(=O)- or - Si(R6)(R7)- and → means bonding with Q1, Q2or Q3}, the remaining one or two of A1, A2and A3are the same or different and each independently represents a group represented by the following formula (3): -R8-a3-R9-a4→{wherein, R8and R9individually represent a single bond or a divalent C1-12hydrocarbon group, a3and a4individually represent a single bond, -S-, -SO-, -SO2-, -SO2NH-, -O-, - N(R10)-, -CON(R11)-, -C(=O)- or -SI(R12)(R13)- and → means bonding with Q1, Q2or Q3},; at least one of Q1, Q2and Q3represents a cyclic hydrocarbon group or heterocyclic group and the remaining one or two of Q1, Q2and Q3individually represent a hydrogen atom, a carboxyl group which may be esterified, a hydrocarbon group or a heterocyclic group] or salt thereof; and a pharmaceutical comprising the same as an effective ingredient. The compound exhibits strong squalene synthetase inhibitory action and is therefore useful as a pharmaceutical for the treatment·prevention of hypercholesterolemia, hyperlipemia or arteriosclerosis.
