High Throughput Bench-Top Co-crystal Screening via a Floating Foam Rack/Sonic Bath Method

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• 作者：Henry Morrison ; Melissa Mrozek-Morrison ; Josh Toschi ; Van Luu ; Helming Tan ; Dominick Daurio
• 刊名：Organic Process Research & Development
• 出版年：2013
• 出版时间：March 15, 2013
• 年：2013
• 卷：17
• 期：3
• 页码：533-539
• 全文大小：553K
• 年卷期：v.17,no.3(March 15, 2013)
• ISSN：1520-586X

文摘

The application of sonication of moist powders in a sonic bath through the use of a floating foam rack was investigated as an inexpensive bench-top high throughput platform for first pass co-crystal screening. The feasibility of this method was tested on two known systems (carbamazepine and AMG 517), and different polymorphic phases of carbamazepine were used as starting material to determine if this had any effect on yielded co-crystal product. This screening method was then applied to two previously unscreened internal molecules, AMG 369 (1) and AMG 277 (2), to determine if co-crystals could be formed for these systems. A high throughput 96-well Symyx co-crystal screen was also run on the internal molecules, and resulting hits for both screens were compared. Several positive hits were scaled up via a twin screw extrusion (TSE) process.