11-Azaartemisinin cocrystals with preserved lactam : acid heterosynthons†,CrystEngComm

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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 ²₂（8）杂 [双键，长度为m-破折号]