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11-Azaartemisinin cocrystals with preserved lactam : acid heterosynthons†
CrystEngComm ( IF 2.6 ) Pub Date : 2018-01-10 00:00:00 , DOI: 10.1039/c7ce01875d
Madiha Nisar 1, 2, 3, 4 , Herman H.-Y. Sung 1, 2, 3, 4 , Horst Puschmann 5, 6, 7, 8 , Richard Lakerveld 2, 3, 4, 9 , Richard K. Haynes 1, 2, 3, 4, 10 , Ian D. Williams 1, 2, 3, 4
Affiliation  

11-Azaartemisinin (11-Aza) is a potent anti-malarial drug more readily able to form cocrystals than its parent compound. 13 new 1 : 1 and 2 : 1 cocrystal phases from 25 mono- and bi-functional acids are reported here in excellent yield and purity by liquid assisted grinding. X-ray structures of several of these cocrystals reveal R22(8) heterosynthons with short OH–O[double bond, length as m-dash]C H-bonds ≤2.60 Å between the 11-Aza lactam and the coformer acid groups. The new phases can show enhanced aqueous solubility of 11-Aza of 3× after 12 h. Notably diastereospecific cocrystal formation can occur, with the DL-mandelic acid system yielding solely the 11-Azaart : D-mandelic acid 1 : 1 product.

中文翻译:

11-氮杂青蒿素与保留的内酰胺共结晶:酸异合子

11-氮杂青蒿素(11-氮杂)是一种有效的抗疟疾药物,比其母体化合物更容易形成共晶体。通过液体辅助研磨,这里报道了由25种单官能和双官能酸形成的13个新的1:1和2:1共结晶相,具有优异的收率和纯度。这些共晶中的几个的X射线结构显示R 2 2(8)杂[双键,长度为m-破折号]合子,在11-氮杂内酰胺和共形成酸基团之间具有短的OH- OC H键≤2.60Å。新相在12小时后可显示出3×的11-Aza水溶性增强。明显地可以发生非对映特异性共晶体,其中DL-扁桃酸体系仅产生11-Azaart:  D-扁桃酸1:1产物。
更新日期:2018-01-10
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