cas 22889-78-7, 4-Amino-3,5-dichloropyridine

Articles about 22889-78-7Total 7 be found

Preparation method of pyridine derivative (by machine translation)
To the method, piperidine-4-one hydrochloride is used as a raw material, and a series of pyridine derivatives are obtained through halogenation reaction and elimination reaction. The reaction is eliminated by reacting piperidine-4-one hydrochloride with a specific amount of the 3,5 - halogenating agent in a halogenation 3, 3, 5 - reaction with a halogen-3, 3, 5, 5 - based reaction, followed by reaction with a pyridine derivative of a hydroxyl group, an amino group 4 - or a dimethylamino group, respectively, by eliminating the reaction with a different kind of basic agent. The method is simple and convenient to operate, mild in condition, short in technological process, low in waste water yield, environment-friendly, low in cost and beneficial to green industrial production of the pyridine derivative. (by machine translation)
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Paragraph 0111-0114

(2019/12/02)

A method for preparing raw material for roflumilast and detection method
The invention discloses a preparation method and a detection method of a roflumilast material. The preparation method comprises the following steps: mixing 3-cyclopropyl methoxy group-4-difluoro methoxy group benzoic acid SM-1, thionyl chloride, dimethyl formamide with toluene, and carrying out an acylating chlorination reaction to obtain a midbody 1; mixing 3,5-dichloro-4-aminopyridine SM-2, tetrahydrofuran with potassium tert-butoxide and carrying out a salt forming reaction to obtain tetrahydrofuran solution of a midbody 2; and then mixing the midbody 1 and the midbody 2 with tetrahydrofuran, carrying out amidation to obtain a crude product of roflumilast, and refining the crude product of roflumilast to prepare the roflumilast material. Aiming to overcome the shortage of the prior art, the preparation process of the roflumilast material is optimized, so that the curative effect for treating diseases such as chronic obstructive pulmonary disease (COPD) is more remarkable; and besides, a systematic, complete and effective composition identifying and content measuring method is provided, so that the quality of the medicine can be effectively controlled, and the clinical effect is ensured.
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Paragraph 0023; 0281-0282

(2018/05/16)

COMPOUNDS CONTAINING PHENYL LINKED TO ARYL OR HETEROARYL BY AN ALIPHATIC- OR HETEROATOM-CONTAINING LINKING GROUP
This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase
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(2008/06/13)

Process development of the PDE IV inhibitor 3-(cyclopentyloxy)-n-(3,5-dichloropyrid-4-yl)-4-methoxybenzamide
Development of an industrial process for 3-(cyclopentyloxy)-N-(3,5-dichloropyrid-4-yl)-4-methoxybenzamide, a potent PDE IV type inhibitor, is described. The rapid identification of scalable reaction conditions allowed pilot-scale synthesis of kilogramme quantities for early clinical evaluation. However, as more compound was demanded, better reaction conditions were required in the interests of safety, economics, and environmental impact. This led to the derivation of a high-yielding and very robust procedure which included various safeguards to ensure that high-quality product was obtained and that new trace impurities were effectively removed. The large-scale oxidation of a benzaldehyde derivative to the corresponding benzoic acid using hydrogen peroxide under aqueous alkaline conditions is described.
Cook, David C.,Jones, Ronald H.,Kabir, Humayun,Lythgoe, David J.,McFarlane, Ian M.,Pemberton, Clive,Thatcher, Alan A.,Thompson, David M.,Walton, John B.
p. 157 - 168
(2013/09/08)

Synthesis of pluriaminated pyridines
The key reagent 3,5-dichloro-4-pyridinecarbonitrile (1) was used to synthesize 4-aminomethylpyridine derivatives 3,5-disubstituted with various amino groups, very active as inhibitors of diamine oxidase. The study of the reaction allowed to discover conditions for the gradual substitution in good yields of the two chlorine atoms to give symmetrically and unsymmetrically disubstituted derivatives (3), or the substitution of the cyano group, or the formation of amidines. The reduction of the cyano to aminomethyl group in compounds (3) afforded the target bioactive products.
De Munno, Angela,Bertini, Vincenzo,Picci, Nevio,Lemma, Francesca,Pocci, Marco
p. 1203 - 1211
(2007/10/03)

Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic-or heteroatom-containing linking group
This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
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(2008/06/13)