162240-96-2Relevant academic research and scientific papers
Preparation method of 2, 6-dimethyl piperazine dihydrochloride
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Paragraph 0073; 0081-0083; 0095; 0100-0101; 0106, (2020/09/21)
The invention provides a preparation method of 2, 6-dimethyl piperazine dihydrochloride, which comprises the following steps: by using N-Boc-alaninamide and propylene oxide as raw materials, carryingout ring-opening reaction, group protection reaction, cyclization reaction and reduction reaction to obtain the 2,6-dimethyl piperazine dihydrochloride. According to the preparation method, when L-N-Boc-alaninamide and R-epoxypropane are used as raw materials, (2S,6S)-2,6-dimethylpiperazine dihydrochloride is prepared, and when D-N-Boc-alaninamide and S-epoxypropane are used as raw materials, (2R,6R)-2,6-dimethylpiperazine dihydrochloride is prepared. The preparation method provided by the invention has the advantages of short synthesis route and mild reaction conditions, and is suitable for industrial production and application.
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist
Hong, Qingmei,Bakshi, Raman K.,Palucki, Brenda L.,Park, Min K.,Ye, Zhixiong,He, Shuwen,Pollard, Patrick G.,Sebhat, Iyassu K.,Liu, Jian,Guo, Liangqin,Cashen, Doreen E.,Martin, William J.,Weinberg, David H.,MacNeil, Tanya,Tang, Rui,Tamvakopoulos, Constantin,Peng, Qianping,Miller, Randy R.,Stearns, Ralph A.,Chen, Howard Y.,Chen, Airu S.,Strack, Alison M.,Fong, Tung M.,MacIntyre, D. Euan,Wyvratt, Matthew J.,Nargund, Ravi P.
scheme or table, p. 2330 - 2334 (2011/05/15)
We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.
PIPERAZINE UREA DERIVATIVES AS MELANOCORTIN-4 RECEPTOR AGONISTS
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, (2010/11/30)
Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders r
Novel piperazine derivatives
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, (2008/06/13)
The present invention is a chemical compound of formula (I) or a pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R4, A1, A2 m and n are as described in the specification.
Asymmetric Synthesis of 2,6-Methylated Piperazines
Mickelson, John W.,Belonga, Kenneth L.,Jacobsen, Jon E.
, p. 4177 - 4183 (2007/10/02)
The complete series of enantiopure 2,6-methylated piperazines was synthesized utilizing two alternative reactions in the key bond-forming step.The dimethyl enantiomers, (2R,6R)- and (2S,6S)-2,6-dimethylpiperazine (1, 2), were prepared using either a diastereoselective triflate alkylation or a novel intermolecular Mitsunobu reaction to set the required stereochemistry.The monomethyl derivatives, (R)- and (S)-tert-butyl 2-methyl-1-piperazinecarboxylate (3, 4) were also synthesized employing the Mitsunobu cyclization strategy while the trimethyl compounds, (R)- and (S)-2,2,6- trimethylpiperazine (5, 6) were prepared using an enantiospecific triflate alkylation as the principal reaction.These methods represent efficient, general strategies for preparing a variety of 2,6-methylated piperazines for which the absolute stereochemistry can be readily controlled.
