公开(公告)号：US5766556A

公开(公告)日：1998-06-16

申请号：US777270

申请日：1996-12-31

申请人： Sheila Helen Hobbs DeWitt ,  John Steven Kiely ,  Michael Raymond Pavia ,  Mel Conrad Schroeder ,  Charles John Stankovic

发明人： Sheila Helen Hobbs DeWitt ,  John Steven Kiely ,  Michael Raymond Pavia ,  Mel Conrad Schroeder ,  Charles John Stankovic

IPC分类号： B01J19/00 ,  C07B61/00 ,  C07C275/28 ,  C07K1/04 ,  C07K5/062 ,  C40B40/06 ,  C40B40/10 ,  C40B50/14 ,  C40B60/14 ,  C08F283/00

CPC分类号： C07K1/047 ,  B01J19/0046 ,  C07K1/045 ,  B01J2219/00283 ,  B01J2219/00308 ,  B01J2219/0031 ,  B01J2219/00373 ,  B01J2219/00416 ,  B01J2219/00423 ,  B01J2219/00454 ,  B01J2219/00493 ,  B01J2219/00495 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00596 ,  B01J2219/00689 ,  B01J2219/00695 ,  B01J2219/0072 ,  B01J2219/00722 ,  B01J2219/00725 ,  C40B40/06 ,  C40B40/10 ,  C40B50/14 ,  C40B60/14

摘要： An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. The apparatus can be adapted to manual, semiautomatic or fully automatic performance. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.

摘要翻译： 提供合适的位置用于多次同时合成化合物的装置和方法。 该装置包括：具有多个井的储存器块; 多个反应管，通常为气体分散管，在其下端具有过滤器; 具有多个孔的保持器块; 以及可以具有允许引入/维护受控环境的端口的歧管。 歧管顶壁具有孔和具有相同孔的可拆卸板。 该装置由适应加热，冷却，搅拌或腐蚀性试剂的材料构成。 垫片放在组件之间。 提供杆或夹具用于将部件固定在一起。 设备操作涉及将过滤器放置在储存器块井中的反应管的下端，并且通过保持器的上端阻挡孔并进入歧管。 该装置提供超过1mg每种产品的结构知识和对每种化合物的控制。 该装置可以适应于手动，半自动或全自动的性能。 使用该装置，一系列构建块共价连接到固体支持物上。 然后通过共价添加其他不同的构建块或化学修饰一些现有功能来修改这些构建块，直到实现倒数第二个结构。 然后通过另一种化学反应将固体支持物从该固体支持物中裂解成孔内的溶液，得到新合成的单独化合物的阵列，其在反应后修饰（如果需要）适于测试活性。