Structural diversity of brexpiprazole and related analogues: Impact on solubility and drug delivery was written by Zeidan, Tarek A.;Tilak, Pranoti A.;Trotta, Jacob T.;Curran, Erin;Oliveira, Mark A.;Chiarella, Renato A.;Almarsson, Orn;Hickey, Magali B.. And the article was included in Crystal Growth & Design in 2018.Recommanded Product: 129722-25-4 This article mentions the following:
Brexpiprazole (BPZ) is an atypical antipsychotic drug indicated for the treatment of schizophrenia and depression. Crystal form screening of BPZ resulted in the formation of three polymorphs (I, II, and III), two methanol solvates, a toluene hemisolvate, and a dihydrate. Thermal anal. and solvent-mediated conversion experiments of the three unsolvated polymorphs established that Form I is the thermodynamically stable form at ambient temperature All three polymorphs are monotropically related, whereby Forms I and II are the most and least stable forms, resp. Structural diversity of BPZ was compared with two chem. related analogs, aripiprazole (APZ) and its active metabolite dehydro-aripiprazole (dAPZ). Like APZ and dAPZ, BPZ was shown to form a thermodynamically stable, hydrated crystal form when exposed to an aqueous environment; however, while APZ and dAPZ were characterized as monohydrates, BPZ is a dihydrate. The crystal structure of BPZ dihydrate (S2H2O) showed two water mols. connecting two BPZ mols., with hydrogen bonding occurring between both the piperazine nitrogen and the oxygen of the carbonyl moiety with different water mols. Despite the chem. similarity of BPZ, APZ, and dAPZ, comparison of all accumulated crystal structures reveals wide structural diversity, with a significant impact on physicochem. properties. In particular, the solubility of BPZ is significantly lower in water across the physiol. relevant pH range. Implications to drug delivery of these findings are discussed. In the experiment, the researchers used many compounds, for example, 7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 129722-25-4Recommanded Product: 129722-25-4).
7-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 129722-25-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. 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.Recommanded Product: 129722-25-4
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics