Application In Synthesis of 1-Methylpiperazine dihydrochlorideOn September 30, 1994 ,《Studies on anti-platelet agents. IV. A series of 2-substituted 4,5-bis(4-methoxyphenyl)pyrimidines as novel anti-platelet agents》 was published in Chemical & Pharmaceutical Bulletin. The article was written by Tanaka, Akito; Motoyama, Yukio; Takasugi, Hisashi. The article contains the following contents:
The syntheses and structure-activity relationships of a series of 2-substituted 4,5-bis(4-methoxyphenyl)pyrimidines, designed on the basis of structural analyses of several cyclooxygenase (CO) inhibitors, and their derivatives as anti-platelet agents based on CO inhibition are described. Among them, 4,5-bis(4-methoxyphenyl)-2-morpholinopyrimidine and 4,5-bis(4-methoxyphenyl)-2-(3,5-dimethylmorpholin-4-yl)pyrimidine showed potent inhibitory activity on malondialdehyde, formed by the CO-catalyzed oxygenation of arachidonic acid (A.A.) in prostanoids, production in vitro (73.4% inhibition at 10-8 M and IC50 = 1.4 × 10-8 M, resp.). Certain compounds were also examined in ex vivo studies. Of these compounds, 4,5-bis(4-methoxyphenyl)-2-(1-methyl-1,2,3,6,-tetrahydropyrid-4-yl)pyrimidine (11a) exhibited potent and long-lasting anti-platelet activity ex vivo, i.e., 11a showed 97% inhibition of platelet aggregation induced by A.A. even 24 h after oral administration of 3.2 mg/kg in guinea pigs, and 60-70% inhibition at 6 h after lower doses (1.0 mg/kg). The ex vivo activity of 11a is more than three times that of aspirin (aspirin showed 81% inhibitory activity on platelet aggregation induced by A.A. at 6 h after oral administration at 10 mg/kg is this study). Compound 11a also showed vasodilatory activity (ED50 = 5.3 × 10-6 M, while aspirin has no vasodilatory activity at 6.0 × 10-4 M). In addition to this study using 1-Methylpiperazine dihydrochloride, there are many other studies that have used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Application In Synthesis of 1-Methylpiperazine dihydrochloride) was used in this study.
1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Application In Synthesis of 1-Methylpiperazine dihydrochloride
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics