A series of salts and binary and ternary cocrystals of the antimalaria drug pyrimethamine (PYR) are reported. PYR has a donor−acceptor−donor (DAD) and a donor−acceptor (DA) binding site, and cocrystallization experiments were performed with coformers with complementary acceptor-donor-acceptor (ADA) and acceptor-donor (AD) H-bonding functionalities. Three different preparation techniques were compared, namely, solution crystallization, crystallization from the gas phase, and liquid-assisted grinding. In several cases different solid-state forms were obtained depending on the crystallization method. The molecular ionic cocrystals PYRH + BAR − •PYR (BAR = barbituric acid) and (PYRH + SAC − ) 2 •GLU (GLU = glutarimide, SAC = saccharin), the binary cocrystal PYR•GLU, the salt PYRH + NIC − (NIC = nicotinic acid), and two polymorphs of PYRH + SAC − could be crystallized by sublimation. Two other ternary molecular ionic cocrystals, (PYRH + BEN − )•PYR•SUC and (PYRH + SAC − ) 2 •SOR (SUC = succinimide, BEN = benzoic acid, SOR = sorbic acid), were obtained by solution crystallization. Attempts to crystallize ternary cocrystals from solution also yielded a number of new twocomponent cocrystals including four new solvates of PYRH + SAC − , thus extending the structural landscape of the PYR/SAC system. Liquid-assisted milling was performed as a one-pot reaction and with the stepwise addition of the coformers. The (PYRH + SAC − ) 2 • GLU cocrystal formed when the coformers were milled in one step and when they were added to the mill stepwise. For other systems the outcome of the two-step milling experiment depended on the order in which the coformers were added. The PYRcoformer interactions were analyzed using the PIXEL program.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
customersupport@researchsolutions.com
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.
Copyright © 2025 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.