1849-53-2Relevant articles and documents
Multi-substituted amine compound and its preparation and use (by machine translation)
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, (2018/04/27)
The invention belongs to the field of medical technology, in particular, the present invention provides the following formula I shown multi-substituted amine compound or its isomer or its pharmaceutically acceptable salt, ester, prodrug or hydrate, its pharmaceutical composition, preparation method thereof and its use in the preparation of medicine for treating aids in use. The compound or pharmaceutical composition containing the compound can be used as an inhibitor for inhibiting HIV integrase with LEDGF/p75 between protein - protein interaction and HIV integrase dimerization, then can be used for the treatment of aids. . (by machine translation)
Stereoselective synthesis of swainsonines from pyridines
Heimg?rtner, Gerres,Raatz, Dirk,Reiser, Oliver
, p. 643 - 655 (2007/10/03)
An efficient synthesis of (-)-swainsonine and (-)-2,8a-di-epi-swainsonine was developed starting from readily available 2-pyridinecarbaldehyde and 3-hydroxypyridine. In particular, it was demonstrated that the mixture of simple indolizidines, i.e. lentigi
SUBSTITUTED 4-AMINO-1-(PYRIDYLMETHYL)PIPERIDINE AND RELATED COMPOUNDS
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Page 65-66, (2010/02/07)
This invention provides 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.
Influence of steric crowding on the electrochemical reduction of substituted tertiary pyridylcarboxamides in aqueous acidic medium
Largeron, Martine,Auzeil, Nicolas,Bacque, Eric,Fleury, Maurice-Bernard
, p. 495 - 501 (2007/10/03)
In order to assess the influence of the steric crowding on the electrochemical reduction of pyridycarboxamides, we have studied a series of tertiary aromatic or alicyclic pyridylcarboxamides. We have shown that increasing steric hindrance at the amide nit
Substituted 6,11-ethano-6,11-dihydrobenzo[b] quinolizinium salts and compositions and methods of use thereof
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, (2015/04/15)
Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: STR1 wherein: R1, R2, R3, R4, R5, R6, R7, X and p are as defined in the specification.
Synthesis and binding properties to GABA receptors of 3-hydroxypyridinyl- and 3-hydroxypiperidinyl-analogues of baclofen
Desideri,Galli,Sestili,Stein
, p. 29 - 33 (2007/10/02)
The synthesis of 3-(3-hydroxy-2-pyridinyl)propanoic acid, 3-(3-hydroxy-2-pyridinyl)-4-aminobutanoic acid, their corresponding piperidine compounds, and of some cyclized derivatives is described. In vitro assays none of the new compounds shows any notewort
Acidity Constants of Benzimidazolium Ketone and Pyridinium Aldehyde Hydrates
Owen, Terence C.
, p. 987 - 990 (2007/10/02)
Acidity constants (pKa) of the hydroxyl groups of the quaternary heterocyclonium carbinols 2-hydroxymethyl-1-methylpyridinium and 2-(1-hydroxyethyl)-1,3-dimethylbenzimidazolium ions are 11.5 +/- 0.5.Acidity constants of the corresponding gem diols, the hydrates of 2-formyl-1-methylpyridinium and 2-acetyl-1,3-dimethylbenzimidazolium ions hence are estimated to be 9 +/- 0.5.Accordingly, acidity constants of the hydroxyl groups of pyridine aldehyde salt hydrates are 12-13, not 4-5 as previously reported; and conversely, acidity constants of the pyridinium groups are 4-5, not 12-13.
Lithiation of Methoxypyridines Directed by α-Amino Alkoxides
Comins, Daniel L.,Killpack, Michael O.
, p. 69 - 73 (2007/10/02)
The addition of methoxypyridinecarboxaldehydes to certain lithium dialkylamides gave α-amino alkoxides in situ that were ring-lithiated with alkyllithium bases.Alkylation and hydrolysis on workup provided ring-substituted methoxypyridinecarboxaldehydes via a one-pot reaction.The one-pot methylation of isomeric methoxypyridinecarboxaldehydes was examined.The regioselectivity of the lithiation-methylation was dependent on the aldehyde, the amine component of the α-amino alkoxide, and the metalation conditions.When lithiated N,N,N'-trimethylethylenediamine was used as the amine component of the α-amino alkoxide, methylation generally occured ortho to the aldehyde function.The analogous reactions using lithium N-methylpiperazide as the amine component gave substitution next to the methoxy group.Several new methylated methoxypyridinecarboxaldehydes were prepared in a regioselective manner by using this one-pot procedure.
ORTHO LITHIATION OF 2-, 3-, AND 4-METHOXYPYRIDINES
Comins, Daniel L.,LaMunyon, Donald H.
, p. 773 - 776 (2007/10/02)
The ortho lithiation of 2-, 3-, and 4-methoxypyridine was effected using mesityllithium as the metalating base.
