Wéber Csaba, Bielik Attila, Szendrei Györgyi I, Keserû György M, Greiner István
Chemical and Biotechnological Research and Development, Gedeon Richter Ltd., PO Box 27, H-1475 Budapest, Hungary.
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1279-81. doi: 10.1016/j.bmcl.2003.12.038.
A readily automated solid-phase approach to the synthesis of diverse N-(phenylalkyl)cinnamides, analogues of the NR2B antagonist 2, is described. The procedure utilizes polymer supported N-(phenylalkyl)amines, (diethylphosphono)acetic acid and a wide range of commercially available hydroxybenzaldehydes. The key step, a Horner-Wadsworth-Emmons reaction is achieved under mild conditions and was found to be general for a large number of benzaldehydes. A 225-member focused library was synthesized using a Tecan Combitec synthesizer.
本文描述了一种易于自动化的固相方法，用于合成多种N-(苯基烷基)肉桂酰胺，即NR2B拮抗剂2的类似物。该方法利用聚合物负载的N-(苯基烷基)胺、(二乙基膦酰基)乙酸和多种市售的羟基苯甲醛。关键步骤，即霍纳尔-沃兹沃思-埃蒙斯反应在温和条件下完成，并且发现对大量苯甲醛具有通用性。使用Tecan Combitec合成仪合成了一个包含225个成员的聚焦文库。
