204316-52-9Relevant academic research and scientific papers
NOVEL PHARMACEUTICAL COMPRISING HETEROAROMATIC AMIDE DERIVATIVE OR SALT THEREOF
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, (2021/09/17)
PROBLEM TO BE SOLVED: To provide a compound useful for treating or preventing disease associated with voltage-dependent sodium channel (Nav1.7) such as disease involving a pain, disease involving an itch, autonomic nerve-associated disease, or a pharmaceutical composition thereof. SOLUTION: The present disclosure provides a compound illustrated by the following formula, and a pharmaceutical composition containing the same. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
NOVEL HETEROAROMATIC AMIDE DERIVATIVE AND MEDICINE CONTAINING SAME
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Paragraph 1024, (2021/07/24)
A compound selectively inhibiting Nav1.7 over Nav1.5 is provided. A heteroaromatic amide derivative or salt thereof showing high efficacy for various diseases associated with Nav1.7 such as pain, represented by the general formula (I) [wherein, X1-X2 is N-C or C-N, Y1 , Y2, Y3 and Y4 are -CH2-, -CR4aH- or -O- and so on, Z1 is-O- and so on, ring A is a 3- to 7-membered monocyclic aromatic ring and so on, R1a and R1b are a hydrogen atom or a halogen atom and so on, R2 is a hydrogen atom and so on, R3a, R3b and R3c are a hydrogen atom or an optionally substituted C1-C6 haloalkyl group and so on, R4a, R4b and R4c are, an optionally substituted C1-C6 haloalkyl group or C1-C6 haloalkoxy group and so on, R5a is a hydrogen atom and so on, R5a and R5b together form -CH2O- and so on, R6a and R6b are a hydrogen atom and so on, n is 1 or 2.].
Syntheses of the four stereoisomers of Phytophthora mating hormone α2 and a concise synthesis of mating hormone α1
Yajima, Arata,Toda, Kou,Molli, Shylaja D.,Ojika, Makoto,Nukada, Tomoo
, p. 8887 - 8894 (2011/12/14)
Four stereoisomers of Phytophthora mating hormone α2 were synthesized using both enantiomers of citronellol as starting materials. The absolute configuration of the natural product was determined to be 7S,11R,15R by oospore-inducing assays of the syntheti
New amino endoperoxides belonging to the antimalarial G-factor series
Givelet, Cecile,Bernat, Virginie,Danel, Mathieu,Andre-Barres, Christiane,Vial, Henri
, p. 3095 - 3101 (2008/02/08)
In the search for new antimalarial endoperoxides we developed a direct route for the preparation of new amino compounds belonging to the G-factor series. During the synthesis, a significant difference in reactivity between two series of diastereoisomers was observed. The final amino endoperoxides were obtained with 58 to 70 % yields, depending on the starting amine, in the "anti" series, but with the "syn" diastereoisomers an unexpected rearrangement occurred during the deprotection step. This was attributed to a transient hexacoordinate fluorosilicon complex allowing the formation of a 1,2-dioxetane. Its decomposition gave aldehyde 12 and 4-hydroxybutan-2-one; these compounds were also identified when acidic conditions were used in the deprotection step. The anti amino compounds obtained were tested, but in vitro activities were found to be lower than initially expected, and fitted poorly with the previous biological hypothesis. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
Emergence of a novel catalytic radical reaction: Titanocene-catalyzed reductive opening of epoxides
Gans?uer, Andreas,Bluhm, Harald,Pierobon, Marianna
, p. 12849 - 12859 (2007/10/03)
The preparatively important catalytic opening of epoxides to β-titanoxy radicals via single-electron transfer (SET) is described. These radicals can be reduced to alcohols or participate in C-C bond-forming reactions. A key step in the catalytic cycle is the conceptually novel protonation of titanium-oxygen and -carbon bonds. Our method combines the advantages of radical reactions, e.g., high functional group tolerance and stability of radicals under protic conditions, with the ability of organometallic complexes to determine the course of transformations in reagent-controlled reactions.
