Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-{2-methoxy-1(R)-4-(trifluoromethyl)phenyl}ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Selective, and Orally Bioavailable CCR5 Antagonist was written by Tagat, Jayaram R.;McCombie, Stuart W.;Nazareno, Dennis;Labroli, Marc A.;Xiao, Yushi;Steensma, Ruo W.;Strizki, Julie M.;Baroudy, Bahige M.;Cox, Kathleen;Lachowicz, Jean;Varty, Geoffrey;Watkins, Robert. And the article was included in Journal of Medicinal Chemistry in 2004.Application of 147081-29-6 This article mentions the following:
The nature and the size of the benzylic substituent are shown to be the key to controlling receptor selectivity (CCR5 vs. M1, M2) and potency in the title compounds Optimization of the lead benzylic Me compound 3 led to the methoxymethyl analog 30, which had excellent receptor selectivity and oral bioavailability in rats and monkeys. Compound 30 (Sch-417690/Sch-D), a potent inhibitor of HIV-1 entry into target cells, is currently in clin. trials. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6Application of 147081-29-6).
(S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Application of 147081-29-6
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics