194350-95-3Relevant articles and documents
Synthesis process for 4-(4-ethyl-4,7-diazaspiro[3,3]octyl)-2-nitroaniline
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Paragraph 0035; 0036, (2018/11/27)
The invention discloses a synthesis process for 4-(4-ethyl-4,7-diazaspiro[3,3]octyl)-2-nitroaniline. The synthesis process comprises the following concrete steps: step 1, reacting 2-piperazinone and aposition-4 nitrogen-protected derivative thereof with ethyl bromide under basic conditions so as to obtain a compound 1; step 2, reacting the compound 1 with a titanium catalyst so as to obtain a compound 2; step 3, subjecting the compound 2 to deprotection to produce the free base 1-ethyl-2-cyclopropyl-piperazine or a hydrochloride thereof; step 4, reacting 1-ethyl-2-cyclopropyl-piperazine or the hydrochloride thereof with a compound 3 so as to obtain a compound 4 is obtained; and step 5, subjecting the compound 4 to deprotection so as to obtain the product 4-(4-ethyl-4,7-diazaspiro[3,3]octyl)-2-nitroaniline. The synthesis process of the invention is simple in synthesis conditions and uses cheap raw materials; and through the selection of a deprotecting agent, the formation of by-products can be reduced, and the yield of the product can be increased, as high as 80%.
PYRAZOLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS
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Page/Page column 88-89, (2014/03/26)
The present disclosure provides compounds of Formula (LA) and/ or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of ty r-osine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and p h ar-maceutically acceptable salts thereof
Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers
Martini, Elisabetta,Ghelardini, Carla,Dei, Silvia,Guandalini, Luca,Manetti, Dina,Melchiorre, Michele,Norcini, Monica,Scapecchi, Serena,Teodori, Elisabetta,Romanelli, Maria Novella
, p. 1431 - 1443 (2008/09/18)
A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity.
