1822-51-1Relevant articles and documents
A 4 - chloromethyl pyridine hydrochloride synthetic method
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, (2019/06/05)
The invention belongs to the field of organic synthesis, in particular to a 4 - chloromethyl pyridine hydrochloride synthetic method, the method comprises the following steps: (1) to 4 - methyl pyridine as raw materials, takes water as a solvent, the potassium permanganate oxide it to 4 - pyridine carboxylic acid, wherein 4 - methyl pyridine with potassium permanganate in a molar ratio of 1: 2.1 - 2.3, the oxidation temperature is 75 - 80 °C, heating 35 min, the reaction is complete the reaction liquid is adjusted to be acidic, and then cooling and filtering to obtain 4 - pyridine carboxylic acid; (2) 4 - pyridine carboxylic acid with methanol under acidic conditions to produce the 4 - pyridine carboxylic acid methyl ester, wherein the 4 - pyridine carboxylic acid with methanol in a molar ratio of 1: 1.3; (3) reduction of 4 - pyridine carboxylic acid methyl ester for 4 - pyridine methanol; (4) 4 - pyridine methanol with thionyl chloride reaction to obtain the target product 4 - chloromethyl pyridine hydrochloride, 4 - pyridine methanol with thionyl chloride in a molar ratio of 1: 1.1 - 1.3.
Tetrazolylhydrazides as selective fragment-like inhibitors of the JumonjiC-domain-containing histone demethylase KDM4A
Rüger, Nicole,Roatsch, Martin,Emmrich, Thomas,Franz, Henriette,Schüle, Roland,Jung, Manfred,Link, Andreas
supporting information, p. 1875 - 1883 (2015/11/10)
The JumonjiC-domain-containing histone demethylase 2A (JMJD2A, KDM4A) is a key player in the epigenetic regulation of gene expression. Previous publications have shown that both elevated and lowered enzyme levels are associated with certain types of cancer, and therefore the definite role of KDM4A in oncogenesis remains elusive. To identify a novel molecular starting point with favorable physicochemical properties for the investigation of the physiological role of KDM4A, we screened a number of molecules bearing an iron-chelating moiety by using two independent assays. In this way, we were able to identify 2-(1H-tetrazol-5-yl)acetohydrazide as a novel fragment-like lead structure with low relative molecular mass (Mr=142 Da), low complexity, and an IC50 value of 46.6 μm in a formaldehyde dehydrogenase (FDH)-coupled assay and 2.4 μm in an antibody-based assay. Despite its small size, relative selectivity against two other demethylases could be demonstrated for this compound. This is the first example of a tetrazole group as a warhead in JMJD demethylases. Anchor fragment: To develop non-promiscuous metalloenzyme inhibitors, a metal-complexing acetohydrazide group was integrated in a tetrazolyl fragment, which can be matured into a scaffold to promote further selectivity at the ligand backbone binding site of these emerging drug targets.
Facile and Selective Synthesis of Chloromethylpyridines and Chloropyridines Using Diphosgene/Triphosgene
Narendar,Gangadasu,Ramesh, Ch.,Raju, B. China,Rao, V. Jayathirtha
, p. 1097 - 1103 (2007/10/03)
Diphosgene and triphosgene in the presence of amines were found to be an excellent chlorinating agents with high selectivity for the preparation of chloromethylpyridines and chloropyridines from picoline-N-oxides and pyridine-N-oxides respectively.
Process for producing arylsulfenyl halide
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Page/Page column 13, (2010/11/29)
A process for producing a compound of the formula (II): wherein Hal1 represents halogen and R1 and R2 each independently represents halogen, alkyl, alkoxy, nitro or cyano, which comprises allowing a halogenating agent to react with a compound of the formula (I): wherein Alk represents branched alkyl and R1 and R2 are as defined above.
Novel 1,4-benzothiazephine and 1,5-benzothiazepine compounds as inhibitors of apical sodium co-dependent bile acid transport and taurocholate uptake
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, (2008/06/13)
Compounds, pharmaceutical compositions, and methods for the treatment of a hyperlipidemic condition in a subject. The compounds of the present invention are apical sodium co-dependent bile acid transport inhibitors and are 1,4-benzothiazepine and 1,5-benzothiazepine compounds corresponding to Formula I: wherein j, m, Y, Z, R1A, R1B, R2A, R2B and R6 are as defined in the specification.
Process for producing imidazole derivatives
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, (2008/06/13)
PCT No. PCT/JP97/04708 Sec. 371 Date Jun. 10, 1999 Sec. 102(e) Date Jun. 10, 1999 PCT Filed Dec. 19, 1997 PCT Pub. No. WO98/29395 PCT Pub. Date Jul. 9, 1998The present invention provides a process for producing a compound of the formula (III): wherein R1 and R3 are independently hydrogen or an organic group; R2 is an organic group; and R4 is an optionally substituted aryl. by reacting the compound of formula (I): wherein R1, R2, and R3 are as defined above, with the compound of formula (II):R4-S-Hal(II)wherein R4 is as defined above and Hal is halogen, in the presence of base.
Indole derivatives as 5-HT1-like agonists
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, (2008/06/13)
Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 is a substituted alkylene; C3 -C7 cycloalkyl optionally substituted with HO; C3 -C6 alkenyl optionally substituted with aryl; C5 -C7 cycloalkenyl; or C3 -C6 alkynyl; R2 is H; halo; F3 C; NC; R8 R9 NOC; a substituted alkylene; R8 R9 NO2 S; R10 S(O)m ; R12 CON(R11); R10 SO2 N(R11); R8 R9 NOCN(R11); R10 O2 CN(R11); R13 (CH2)n CH=CH; or R7 O are selective 5-HT1 -like receptor agonists useful in the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.
4-Phenoxymethyl-piperidines
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, (2008/06/13)
4-Phenoxymethyl-piperidines of the formula STR1 wherein R is hydrogen, halogen, nitro, lower alkyl or lower alkoxy, in the form of the free base or an acid addition salt, are provided and they are useful as intermediates in the production of anti-hypertensive agents through condensation with (a) propyl chloride and then with an adenine, or (b) a propyl indole.
