cas 6636-55-1, 6-CHLORO-2-PICOLINIC ACID METHYL ESTER

Articles about 6636-55-1Total 15 be found

Gas chromatographic assay and disposition of 6-chloro-2-pyridylmethyl nitrate, a new antianginal drug, in healthy volunteers
Quantitative determinations of plasma concentrations of 6-chloro-2-pyridylmethyl nitrate, a new antianginal drug, and its urinary metabolite, 6-chloro-2-pyridinecarboxylic acid (metabolite 1), were obtained using GC with a 63Ni electron-capture detector. 6-Chloro-2-pyridylmethyl nitrate was extracted from plasma with n-pentane. Metabolite 1 was extracted from acidic urine with ethylacetate, back extracted with 0.1 M NaHCO3, and methylated with boron trifluoride methanol reagent. The internal standard for metabolite 1 determination was prepared by propylation of metabolite 1 with boron trifluoride n-propanol reagent. The formation of the esters was confirmed by the GC-MS results. These methods proved to be sensitive and reproducible. A single dose of 6-chloro-2-pyridylmethyl nitrate (5, 10, 20, 40, or 60 mg) was given perorally to healthy volunteers. From the data, a large interindividual variability in the apparent plasma clearance was apparent (85.5 ± 123 L/min; CV 144%). However, metabolite 1 was the main metabolite in human urine, and the interindividual variation was slight (CV 13%).
Terada,Sakata,Ishibashi,Tsuchiya,Noguchi,Sugiyama,Nonoyama,Nakashima,Kanamaru
p. 206 - 210
(1989)
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N,6-BIS(ARYL OR HETEROARYL)-1,3,5-TRIAZINE-2,4-DIAMINE COMPOUNDS AS IDH2 MUTANTS INHIBITORS FOR THE TREATMENT OF CANCER
Provided are compounds of formula (I), Wherein: ring A and ring B are each independently an optionally substituted 5-6 membered monocyclic aryl or heteroaryl. The compounds are inhibitors of isocitrate dehydrogenase 2 (IDH2) mutants useful for treating cancer.
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Page/Page column 52; 53

(2015/02/02)

THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
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Page/Page column 117

(2013/07/19)

CXCR4 RECEPTOR ANTAGONISTS
The compounds of formula (I) are antagonists of the CXCR4 receptor Wherein R1, X, Y and R2 are as defined in the claims.
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Page/Page column 37

(2012/05/04)

NOVEL INHIBITORS OF PROTEIN KINASE
The present invention relates to novel compounds for inhibition of angiogenesis receptor tyrosine kinases, in particular, VEGF receptor 2 kinase ("KDR") activity, and preparations for preparation of them, and the use of them, and pharmaceutical compositions containing them at a therapeutically effective amount. The compounds according to the present invention are useful for the treatment and prevention of diseases resulting from the undesired KDR activity, for example, angiogenesis-related diseases such as cancers, psoriasis, rheumatoid arthritis, diabetic retinopathy, etc.
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Page/Page column 47

(2010/11/27)

THIOXANTHINE DERIVATIVES AND THEIR USE AS INHIBITORS OF MPO
There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.
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Page/Page column 73-74

(2008/06/13)

Reaction of N-fluoropyridinium fluoride with isonitriles: A convenient route to picolinamides
Reaction of N-fluoropyridinium fluoride generated in situ with a series of isonitriles led to the formation of the corresponding picolinamides in good yields. A similar reaction sequence for quinoline yielded the respective derivatives of 2-quinoline carboxylic acid. The proposed reaction mechanism involves the intermediate formation of a highly reactive carbene species.
Kiselyov, Alexander S.
p. 2279 - 2282
(2007/10/03)

Selective palladium-catalysed carbonylations of dichloroquinoline and simple dichloropyridines
Dichloroquinoline and some dichloropyridines undergo selective alkoxycarbonylation in the presence of carbon monoxide, an alcohol and PdCl2(PPh3)2 as a catalyst, affording chloro-monoester and/or diesters in good yields under selected reaction conditions.
Najiba, Douja,Carpentier, Jean-Francois,Castanet, Yves,Biot, Christophe,Brocard, Jacques,Mortreux, Andre
p. 3719 - 3722
(2007/10/03)

Synthesis of a tritium labelled analog of the novel hematoregulatory agent SB 209978
[3H]-SB 209978 (10) was synthesized in 6 steps from phenylene diamine dihydrochloride. A key aspect was the regioselective synthesis of 6-chloropicolinic acid (7). This was condensed with diamine 6 and the resulting product was deprotected to give 9. Palladium catalyzed 3H-hydrogenolysis of the chloropyridine rings gave the final produce 10.
Heerding, Dirk,Saunders, David
p. 455 - 460
(2007/10/03)

Preparation of substituted 2-chloropyridines
A process for the preparation of a substituted 2-chloropyridine derivatives of the formula STR1 in which R1, R2, R3 and R4 represent hydrogen or various other radicals, which comprises reacting a pyridine-1-oxide of the formula STR2 with an aromatic carbonyl chloride in the presence of an inert organic solvent and in the presence of an acid acceptor at a temperature between about -20° C. and 200° C.
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(2008/06/13)

Process for the preparation of substituted 2-chloropyridines
A new process has been found for the preparation of substituted 2-chloropyridine derivatives of the formula (I) STR1 wherein R1 to R4 have the meanings as defined in the description. The new process is characterized in that pyridine 1-oxides of the formula II STR2 are reacted with a chlorine-containing phosphoric acid derivative from the series of the chlorophosphoric esters and chlorophosphoramides in the presence of an inert organic solvent and in the presence of an acid acceptor at temperatures between -20° C. and 200° C., and the resulting product is separated further, if appropriate. Compound (I) is known as an intermediate product for medicaments (cf.DE-A 2,812,585) or for insecticidel nitromethylene derivatives (cf. EP-A 163,855).
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(2008/06/13)

THE METHYLATION OF CARBOXYLIC ACIDS USING METHYL TRICHLOROACETATE
Metyl trichloroacetate has been shown to methylate carboxylic acids with the loss of chloroform and carbon dioxide.
Renga, James M.,Wang, Pen-Chung
p. 77 - 82
(2007/10/02)

POLYORGANOMETALLIC HETEROCYCLES. 2,6-DILITHIOPYRIDINE
Metal-halogen exchange between 2,6-diiodo- and 2,6-dibromopyridine and two equivalents of n-butyllithium gives 2,6-dilithiopyridine.On quenching with either carbon dioxide followed by esterification, methanol or dimethyl disulfide the dilithio compound gives a methyl 2,6-pyridinedicarboxylate, pyridine, or 2,6-dithiomethylpyridine, respectively.A convenient procedure for halogen-halogen exchange is also described.
Newkome, George R.,Roper, Jerry M.
p. 147 - 153
(2007/10/02)