- ARYL-N-ARYL DERIVATIVES FOR TREATING A RNA VIRUS INFECTION
-
The present invention relates to a compound of formula (I) wherein X1 represents an alkenylene group, a -NH-CO- group, a -CO-NH- group, Y1 represents an aryl group selected from a pyridyl group, a pyrazinyl group or a pyrimidinyl group, X2 represents a -O- group, a-CO-NH- group, a -NH-CO-NH- group, a -OCH2- group, a -NH-CO- group, a divalent 5-membered heteroaromatic ring comprising 1, 2, 3 or 4 heteroatoms or a -SO2-NH- group, and Y2 represents a hydrogen atom, a hydroxyl group, a morpholinyl group, a piperidinyl group, optionally substituted by a (C1-C4)alkyl group, a piperazinyl group, optionally substituted by a (C1-C4)alkyl group, or a -CR1R2R3 group or alternatively X2-Y2 represents a group -CONRcRd, wherein Rc and Rd form, together with the nitrogen atom a heterocyclic ring, optionally substituted by one or two (C1-C4)alkyl group, by a cyclopentyl group thus forming a spirocyclopentyl, or by a trifluoromethyl group, or any of its pharmaceutically acceptable salt, for use in the treatment and/or prevention of a RNA virus infection caused by a RNA virus belonging to group IV or V of the Baltimore classification. The present invention further relates to new compounds, to pharmaceutical compositions containing them and to synthesis process for manufacturing them.
- -
-
Page/Page column 51-52
(2020/02/06)
-
- Direct Wittig Olefination of Alcohols
-
A base-promoted transition metal-free approach to substituted alkenes using alcohols under aerobic conditions using air as the inexpensive and clean oxidant is described. Aldehydes are relatively difficult to handle compared to corresponding alcohols due to their volatility and penchant to polymerize and autoxidize. Wittig ylides are easily oxidized to aldehydes and consequently form homo-olefination products. By the strategy of simultaneously in situ generation of ylides and aldehydes, for the first time, alcohols are directly transferred to olefins with no need of prepreparation of either aldehydes or ylides. Thus, the di/monocontrollable olefination of diols is accomplished. This synthetically practical method has been applied in the gram-scale synthesis of pharmaceuticals, such as DMU-212 and resveratrol from alcohols.
- Li, Qiang-Qiang,Shah, Zaher,Qu, Jian-Ping,Kang, Yan-Biao
-
p. 296 - 302
(2018/02/19)
-
- C(sp3)-H functionalization of methyl azaarenes: a calcium-catalyzed facile synthesis of (E)-2-styryl azaarenes and 2-aryl-1,3-bisazaarenes
-
Alkaline earth (Ca2+) catalyzed sp3 C-H functionalization of methyl azaarenes for the synthesis of biologically important (E)-2-styryl azaarenes, 2-aryl-1,3-bisazaarenes and 3,3-bisazaarenyl indolinones has been described. Initially methyl azaarenes react with aryl aldehydes to give β-hydroxy derivatives, which undergo Ca(II) catalyzed thermodynamic elimination to give the styryl azaarenes in a single step. Similarly it may undergo SN1 reaction to give 2-aryl-1,3-bisazaarenes and 3,3-bisazaarenyl indolinones (if isatin used as the electrophile). This green synthetic methodology enjoys the simple reaction procedures, solvent free conditions, step economy, substrate diversity and high yields of the products in short time.
- Yaragorla, Srinivasarao,Singh, Garima,Dada, Ravikrishna
-
supporting information
p. 5924 - 5929
(2015/11/02)
-
- Palladium complex of 6-(2-hydroxy-5-methylphenyl)-3-(pyridin-2-yl)-1,2,4- triazin-5(2H)-one: Synthesis, structure, and catalytic activity
-
Palladium(II) complex with 6-(2-hydroxy-5-methylphenyl)-3-(pyridin-2-yl)-1, 2,4-triazin-5(2H)-one was synthesized for the first time. The ligand was prepared from 3-(pyridin-2-yl)-1,2,4-triazin-5(2H)-one and 4-methylphenol via nucleophilic substitution of hydrogen (SNH reaction). The complex was readily soluble in basic medium, and it effectively catalyzed Mizoroki-Heck reaction. Pleiades Publishing, Ltd., 2011.
- Mekhaev,Pestov,Slepukhin,Yatluk,Pervova,Samorukova,Chupakhin
-
experimental part
p. 1366 - 1369
(2011/12/04)
-
- Heterocyclic ethenyloxanilates as orally active antiallergic agents
-
Ethyl p-(pyrimidin-4-ylethenyl)oxanilate 2 and many substituted derivatives were found to have oral activity in the PCA assay. The pyrimidine moiety was replaced by other heterocycles but only pyrazine and pyridazine retained activity.
- Grozinger,Sorcek,Oliver
-
p. 487 - 491
(2007/10/02)
-
- Reactions of Lithio Trimethylsilyl Compounds with Nitrones
-
The reactions of lithio compounds, generated in situ from 2-pyridine (1), N,N-dimethyl(trimethylsilyl)acetamide (2), and ethyl (trimethylsilyl)acetate (3) and LDA in THF, with various nitrones have been investigated.The lithio compounds of 1-3 reacted with α,N-diarylnitrones to give the corresponding (E)-alkenes together with azoxybenzene and/or azobenzene.On the other hand, the reaction of lithio derivative of 1 with α-aryl-N-alkylnitrones, α,N-dialkylnitrones, and cyclic nitrones afforded the aziridine compounds as the major products, accompanied by hydroxylamine derivatives in some cases.The lithio derivative of 2 or 3 reacted with α,N-dialkylnitrones and cyclic nitrones to give the aziridine and/or isoxazolidinone derivatives.The pathways for the formation of the above products are also described.
- Tsuge, Otohiko,Sone, Kazuhiro,Urano, Satoshi,Matsuda, Koyo
-
p. 5171 - 5177
(2007/10/02)
-
- REACTIONS OF SILYL-SUBSTITUTED CARBANIONS WITH NITRONES
-
The reaction of carbanions, prepared from 2-(trimethylsilylmethyl)pyridine or N,N-dimethyltrimethylsilylacetamide and lithium diisopropylamide in tetrahydrofuran, with α-aryl-N-phenylnitrones afforded a mixture of corresponding (E)-alkene, azobenzene and azoxybenzene, respectively.On the other hand, the carbanions reacted with cyclic nitrones to give the corresponding aziridine and/or hydroxylamine derivatives as major products.
- Tsuge, Otohiko,Sone, Kazuhiro,Urano, Sathoshi
-
p. 977 - 980
(2007/10/02)
-