1701-69-5Relevant academic research and scientific papers
Casein kinase 1 (CK1) inhibitor for plants (by machine translation)
-
, (2020/02/14)
[Problem] to provide various lead compounds PHA derivatives, and/or circadian rhythm control agent having stronger CK1 inhibitor activity. [Solution] a compound represented by formula I, or a salt thereof or a solvate thereof. (R1 The, H or C1 - 5 A straight-chain, branched or cyclic alkyl group, alkenyl group or alkynyl group, R2 The, H, halogen (F, Cl, Br or I), or a C1 - 4 The alkyl group, the ring A, 5 - 8 membered lactam ring showing; however, R1 And R2 Except H together. )[Drawing] no (by machine translation)
Chloroacetate-promoted selective oxidation of heterobenzylic methylenes under copper catalysis
Liu, Jianming,Zhang, Xin,Yi, Hong,Liu, Chao,Liu, Ren,Zhang, Heng,Zhuo, Kelei,Lei, Aiwen
supporting information, p. 1261 - 1265 (2015/01/30)
The efficient selective oxidation and functionalization of C-H bonds with molecular oxygen and a copper catalyst to prepare the corresponding ketones was achieved with ethyl chloroacetate as a promoter. In this transformation, various substituted N-heterocyclic compounds were well tolerated. Preliminary mechanistic investigations indicated that organic radical species were involved in the overall process. The N-heterocyclic compounds and ethyl chloroacetate work synergistically to activate C-H bonds in the methylene group, which results in the easy generation of free radical intermediates, thus leading to the corresponding ketones in good yields.
Comparative inhibition of tetrameric carbonyl reductase activity in pig heart cytosol by alkyl 4-pyridyl ketones
Shimada, Hideaki,Tanigawa, Takahiro,Matayoshi, Kazunori,Katakura, Kazufumi,Babazono, Ken,Takayama, Hiroyuki,Murahashi, Tsuyoshi,Akita, Hiroyuki,Higuchi, Toshiyuki,Eto, Masashi,Imamura, Yorishige
, p. 397 - 400 (2014/06/09)
Context and objective: The present study is to elucidate the comparative inhibition of tetrameric carbonyl reductase (TCBR) activity by alkyl 4-pyridyl ketones, and to characterize its substrate-binding domain. Materials and methods: The inhibitory effect
Facile conversion of pyridine propargylic alcohols to enones: Stereochemistry of protonation of allenol
Erenler, Ramazan,Biellmann, Jean-Fran?ois
, p. 5683 - 5685 (2007/10/03)
The conversion of 4-pyridyl propargylic alcohols 1 to the (E)-propenones 3 and propynones 2 occurs under mild reaction conditions, pyridinium chloride in methanol at room temperature. (Z)-4-Pyridyl propenones 11 are detected as initial products when large
The anion of 3-methyl-2-pyridin-4-yl-1,3-oxazine
Sheldrake, Peter,Tyrrell, Elizabeth,Mintias, Shirin,Shahid, Imran
, p. 2263 - 2268 (2007/10/03)
n-Butyllithium at -78°C readily abstracts the methine proton from the title compound. The anion reacts efficiently with a range of electrophiles to provide 4-pyridyl ketones upon acid hydrolysis.
Syntheses of indoloquinolizidines through isomerisation and cyclisation of seco-precursors.
Massiot, G.,Cherif, A.
, p. 648 - 655 (2007/10/02)
The NaBH4 reduction of the salts made from tryptophyl bromide and various pyridines are cyclised according to two procedures which imply shifts of double bonds or transformation of allylic amines into enamines.The first method is an extension of the Barton and Grieco processes in which alkenes are isomerised in the presence of rhodium-III salts.The second method is an acid induced deconjugation of α,β-unsaturated ketones and aldehydes with trapping of incipient iminium ions by indole nuclei.These techniques have allowed preparation of intermediates en route to syntheses in the antirhine series; the rhodium induced cyclisation permitted exclusive preparation of the trans isomer of deethylvincamone.Reaction of vinylmagnesium bromide with 4-formylpyridine yields 4-propionylpyridine in a single step.
5-Heteroarylimidazol-2-ones having cardiotonic activity
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, (2008/06/13)
Described are compounds of the formula STR1 wherein R is heteroaryl and R1 is hydrogen or loweralkyl, or a pharmaceutically acceptable salt thereof. The compounds exhibit cardiotonic activity.
The synthesis of 2-amino-4-(4-imidazolyl)pyridines
LaMattina
, p. 533 - 538 (2007/10/02)
A general synthetic scheme for the preparation of 2-amino-4-(4-imidazolyl)pyridines, potential histamine H2 antagonists, is described. The synthesis is based on the Neber rearrangement of 1-(4-pyridyl)-l-alkanone oxime O-tosylates to the appropriate α-aminoketones or α-aminoketals, which are then converted to the corresponding imidazoles. The reaction of Grignard reagents with 2-chloroisonicotinonitrile, as well as nucleophilic displacement of chloride by amines on 2-chloroisonicotinonitrile and derivatives, are discussed in relation to the preparation of the ketone intermediates.
Ligand interaction of sustituted pyridines with cytochrome P-450.
Born,Early
, p. 850 - 851 (2007/10/02)
A series of pyridyl ketones and alkyl pyridines was evaluated as type II ligands for cytochrome P-450. Activity as type II ligands was evaluated in terms of the lipid solubility and the pKa values of the compounds.
