- DITERPENOID COMPOUNDS THAT ACT ON PROTEIN KINASE C (PKC)
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This present disclosure relates to protein kinase C (PKC) modulating compounds, methods of treating a subject with cancer using the compounds, and combination treatments with a second therapeutic agent.
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- Palladium-Catalyzed Synthesis of Alkynes via a Tandem Decarboxylation/Elimination of (E)-Enol Triflates
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A mild catalytic synthesis of alkynes via a tandem Pd-catalyzed decarboxylation/elimination of enol triflates is described. Key attributes of the method include readily available starting materials, broad functional group tolerance, and the ability to access terminal, internal, and halogenated alkynes. The preliminary scope of the reaction is demonstrated on 25 different examples with yields ranging from 63% to 96%.
- Munteanu, Charissa,Frantz, Doug E.
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supporting information
p. 3937 - 3939
(2016/08/30)
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- A Sequential Homologation of Alkynes and Aldehydes for Chain Elongation with Optional 13C-Labeling
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Terminal alkynes (RCCH) are homologated by a sequence of ruthenium-catalyzed anti-Markovnikov hydration of alkyne to aldehyde (RCH2CHO), followed by Bestmann-Ohira alkynylation of aldehyde to chain-elongated alkyne (RCH2CCH). Inverting the sequence by starting from aldehyde brings about the reciprocal homologation of aldehydes instead. The use of 13C-labeled Bestmann-Ohira reagent (dimethyl ((1-13C)-1-diazo-2-oxopropyl)phosphonate) for alkynylation provides straightforward access to singly or, through additional homologation, multiply 13C-labeled alkynes. The labeled alkynes serve as synthetic platform for accessing a multitude of specifically 13C-labeled products. Terminal alkynes with one or two 13C-labels in the alkyne unit have been submitted to alkyne-azide click reactions; the copper-catalyzed version (CuAAC) was found to display a regioselectivity of >50 000:1 for the 1,4- over the 1,5-triazine isomer, as shown analytically by 13C NMR spectroscopy.
- Brunner, Andreas,Hintermann, Lukas
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supporting information
p. 2787 - 2792
(2016/02/27)
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- Manganese(III)-mediated selective diphenylphosphinoyl radical reaction of 1,4-diaryl-1-butynes for the synthesis of 2-phosphinoylated 3,4- dihydronaphathalenes
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A diphenylphosphinoyl radical-initiated sequential reaction of 1,4-diaryl-1-butynes and analogues is developed for the synthesis of 2-phosphinoylated 3,4-dihydronaphathalenes and related compounds.
- Li, Da-Peng,Pan, Xiang-Qiang,An, Li-Tao,Zou, Jian-Ping,Zhang, Wei
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p. 1850 - 1855
(2014/03/21)
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- Directing group-controlled hydrosilylation: Regioselective functionalization of alkyne
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Pt(0)-catalyzed hydrosilylation of unsymmetric alkynes proceeds in a highly regioselective manner with a dimethylvinylsilyl (DMVS) group as the directing group. This hydrosilylation affords a single regioisomer of silylalkenes from propargylic and homopro
- Kawasaki, Yuuya,Ishikawa, Youhei,Igawa, Kazunobu,Tomooka, Katsuhiko
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supporting information; experimental part
p. 20712 - 20715
(2012/02/15)
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- Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors
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The present study identified several 4-alkynyl and 4-alkenylquinazolines that serve as novel and potent EGFR tyrosine kinase inhibitors. The IC50 values of these compounds are in the nanomolar range. In addition, the 4-(4-phenylbut-1-yn/en-yl)q
- Kitano, Yasunori,Suzuki, Tsuyoshi,Kawahara, Eiji,Yamazaki, Takahisa
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p. 5863 - 5867
(2008/04/03)
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- AMINO ALCOHOL DERIVATIVE OR PHOSPHONIC ACID DERIVATIVE AND MEDICINAL COMPOSITION CONTAINING THESE
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The present invention relates to amino alcohol derivatives or phosphonic acid derivatives having excellent immunosuppressive activity, pharmacologically acceptable salts thereof or pharmacologically acceptable esters thereof, and to pharmaceutical compositions comprising said compounds as an active ingredient: [wherein, ???R1 and R2 each represent a hydrogen atom, or a protecting group of the amino group; ???R3 represents a hydrogen atom, or a protecting group of the hydroxyl group; ???R4 represents a lower alkyl group; ???n represents an integer of from 1 to 6; ???X represents an oxygen atom or a nitrogen atom unsubstituted or substituted with a lower alkyl group or the like; ???Y represents an ethylene group; ???Z represents a C1-C10 alkylene group; ???R5 represents an aryl group, or an aryl group substituted with substituents; ???R6 and R7 each represents a hydrogen atom; provided that when R5 represents a hydrogen atom, then Z represents a group other than a single bond or a straight chain C1-C10 alkylene group] .
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- AMINO ALCOHOL DERIVATIVES
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The present invention relates to compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof, esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 alkylene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 alkylene group.
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- Amino alcohol derivatives
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Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof, esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 alkylene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 alkylene group.
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- Borane-induced radical reduction of 1-alkenyl- and 1-alkynyl-λ3-iodanes with tetrahydrofuran
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Exposure of 1-alkenyl(phenyl)- and 1-alkynyl(phenyl)-λ3-iodanes to THF at room temperature in the presence of a catalytic amount of trialkylborane results in smooth reduction to give 1-iodo-1-alkenes and 1-iodo-1-alkynes as major products, respectively. The key step in the reductions probably involves a single-electron transfer from α-tetrahydrofuryl radical to the λ3-iodanes, which generates the labile [9-I-2] iodanyl radicals.
- Ochiai, Masahito,Tsuchimoto, Yoshimi,Hayashi, Takanori
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p. 5381 - 5384
(2007/10/03)
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- Piperidino-hydrocarbon compounds as novel non-imidazole histamine H3-receptor antagonists
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In search for novel non-imidazole histamine H3-receptor antagonists, piperidino-hydrocarbon compounds were synthesized using the known non-imidazole histamine H3-receptor antagonist FUB 637 (3-phenylpropyl 3-piperidinopropyl ether) as lead structure. Piperidino-alkyl derivatives containing highly flexible side chains (2, 4-7) were prepared via N-alkylation. Compounds containing unsaturated alkyl groups were synthesized in order to investigate the impact of rigidifying the side chain (8-16). Terminal alkynes were prepared by alkylation of lithium acetylide-ethylenediamine complex, disubstituted alkynes were synthesized by alkylation of the appropriate acetylene in the presence of n-butyllithium-N,N,N′,N′-tetramethylene-ethylene-diamine complex. The novel compounds were investigated in an in vitro functional assay on the guinea-pig ileum, in which N-(7-phenylhept-3-ynyl)piperidine (14) proved to be of good potency in this class (pA2=7.21). In an in vivo assay the compounds were additionally screened for their abilities to influence central H3-histaminergic neuron activity in mice with regard to their oral availabilities and distribution properties. In this screening, N-pent-4-ynylpiperidine (9) and N-hex-5-ynylpiperidine (10) proved to be highly potent and orally available histamine H3-receptor antagonists. The ED50 values for 9 and 10 were 1.3 and 1.4 mg/kg po, respectively, which is in the potency range of the reference antagonist thioperamide.
- Meier, Galina,Ligneau, Xavier,Pertz, Heinz H,Ganellin,Schwartz, Jean-Charles,Schunack, Walter,Stark, Holger
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p. 2535 - 2542
(2007/10/03)
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- Formamides undergo in-plane bimolecular nucleophilic vinylic substitutions (S(N)2) by the reaction with (E)-alkenyl(phenyl)iodonium tetrafluoroborates: Stereoselective synthesis of (Z)-vinyl formates
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Reported for the first time is the stereoselective synthesis of (Z)-vinyl formates, which involves in-plane bimolecular nucleophilic vinylic substitutions of (E)-β-alkylvinyl(phenyl)iodonium tetrafluoroborates with formamides.
- Ochiai, Masahito,Yamamoto, Shinji,Sato, Koichi
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p. 1363 - 1364
(2007/10/03)
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- UROKINASE INHIBITORS
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Disclosed are benzothiophene and thienothiophene derivatives useful for inhibiting urokinase activity.
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- PALLADIUM-CATALYZED REDUCTION OF PROPARGYLIC ACETATES WITH SmI2. A MILD AND CONVENIENT METHOD FOR THE PREPARATION OF ALLENES
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A highly regioselective reduction of propargylic acetates has been attained by using SmI2 and catalytic Pd(0) in the presence of 2,4-dimethyl-3-pentanol affording various types of allenes in high yields.
- Tabuchi, Takanori,Inanaga, Junji,Yamaguchi, Masaru
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p. 5237 - 5240
(2007/10/02)
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- A NEW METHOD FOR THE CONVERSION OF ALDEHYDES (RCH2CHO) TO ACETYLENES (RC*CH) VIA 1-ALKENYLSTANNANES. APPLICATION TO THE SYNTHESIS OF 9(O)-THIA-Δ6-PGI1
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A method for the conversion of aldehydes to acetylenes via 1-alkenylstannanes is reported, including its application to the synthesis of 9(O)-thia-Δ6-PGI1.
- Shibasaki, Masakatsu,Torisawa, Yasuhiro,Ikegami, Shiro
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p. 4607 - 4610
(2007/10/02)
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