13484-40-7Relevant articles and documents
N - alkylpiperazine purification of
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Paragraph 0056, (2017/02/28)
PROBLEM TO BE SOLVED: To provide a purification method of N-alkyl piperazines, capable of providing high purity N-alkyl piperazines with low cost and having a high recovery rate.SOLUTION: A mixture of N-alkyl piperazines and a piperazine is distilled in the presence of a polar organic solvent having a higher boiling point than that of the piperazine.
Method for producing N-alkylpiperazine
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Paragraph 0056; 0059, (2017/02/09)
PROBLEM TO BE SOLVED: To provide a method for producing N-alkyl piperazines in high yield by selectively alkylating one amino group.SOLUTION: In the method for producing N-alkyl piperazines, piperazines represented by general formula (1) are reacted with a specific alkylating agent in the presence of an acid. In the formula: R-Rare each independently a hydrogen atom, a methyl group, an ethyl group, a 3-8C linear alkyl group or the like, a hydroxyethyl group, a hydroxypropyl group, a dihydroxypropyl group, a methoxy group, an ethoxy group, a phenyl group, a benzyl group, a 2-phenylethyl group, or the like.
2,5-Disubstituted pyridines as potent GPR119 agonists
Wu, Yulin,Kuntz, Judith D.,Carpenter, Andrew J.,Fang, Jing,Sauls, Howard R.,Gomez, Daniel J.,Ammala, Carina,Xu, Yun,Hart, Shane,Tadepalli, Sarva
scheme or table, p. 2577 - 2581 (2010/06/19)
A series of 2-piperazinyl-5-alkoxypyridines were synthesized and screened against human GPR119 receptor. Through SAR analysis, compounds containing 2-alkylsulfonylpiperazinyl-5-alkoxypyridines were discovered and found to be potent agonists of the human GPR119 receptor.
Discovery and biological evaluation of adamantyl amide 11β-HSD1 inhibitors
Webster, Scott P.,Ward, Peter,Binnie, Margaret,Craigie, Eilidh,McConnell, Kirsty M.M.,Sooy, Karen,Vinter, Andy,Seckl, Jonathan R.,Walker, Brian R.
, p. 2838 - 2843 (2008/02/05)
A series of adamantyl amide 11β-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11β-HSD1 over 11β-HSD2 and possess excellent cellular potency in human and murine 11β-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.
Pyrrolidinone derivatives
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, (2008/06/13)
Since a compound represented by general formula (1), its pharmaceutically acceptable salt and a hydrate of the pharmaceutically acceptable salt have high antipsychotic activity, they may be used as an active ingredient for preparation of an antipsychotic. STR1 Also provided are an optical resolution method of the above compound and an intermediate for preparation of the compound.
Synthesis and biological activity of 3'-hydroxy-5'-aminobenzoxazinorifamycin derivatives
Yamane,Hashizume,Yamashita,Konishi,Hosoe,Hidaka,Watanabe,Kawaharada,Yamamoto,Kuze
, p. 148 - 155 (2007/10/02)
As a part of our studies on the syntheses of benzoxazinorifamycin derivatives, 3'-hydroxy-5'-aminobenzoxazinorifamycin derivatives were synthesized, and tested for their antimicrobial activities. The antimicrobial activities of these compounds against gram-positive and gram-negative bacteria were almost identical to those of rifampicin (RFP) and rifabutain (RFB), however, antimicrobial activities against Mycobacterium tuberculosis were superior to RFP, while being similar to RFB. 3'-Hydroxy-5'-(4-alkyl-1-piperazinyl)benzoxazinorifamycin derivatives also had in vitro potent activities against Mycobacterium avium complex (MAC). Their minimal inhibitory concentration values against MAC were 2-256 times greater than RFP and RFB. Their in vivo efficacies against M. tuberculosis and MAC, after oral administration to mice, were superior to RFP and REB, except for RFB against M. tuberculosis activity in vivo. Although they were absorbed from the gastrointestinal tract, their plasma levels were lower than that of RFP. Among these 5'-(4-alkyl-1-piperazinyl) derivatives, 3'-hydroxy-5'-(4-isobutyl-1-piperazinyl)benzoxazinorifamycin, compound 19 (KRM-1648), was selected as the most promising and its preliminary pharmacokinetic characteristics in mice were investigated. Compound 19 was distributed much more in tissues, especially in spleen and lung, than in plasma and had a long elimination time from tissues.