SYNTHESIS OF PEPTIDE AND NONPEPTIDE OPIOID ANALOGS

描述：(改编自申请人的摘要)固相 科学公司(SPSC)提议建立一个图书馆， 七肽类似物和烷基醚取代物库 靶向Delta和k(Kappa)阿片的吡咯烷胺类似物 感受器。这两个复合库将分别包含2-5毫克 总共有192种化合物。SPSC将通过利用 它是一种新型的高负载顺磁支架，是一种商用的 可用的溶剂输送机器人。具体地说，将制作库 离开这个高负荷的顺磁支架，利用超声波来 协助反应的混合和运行。恒定磁场 将使用字段将载体与可溶组分分开 反应混合物的浓度。将使用液体搬运机器人来添加 试剂和溶剂，并通过吸除废溶剂。 第一阶段工作的目标将是整合声学， 磁选与自动化液体处理合二为一 产生由多肽和非多肽组成的文库的系统 用于阿片受体筛选的化合物。

DESCRIPTION: (Adapted from the applicant's abstract) Solid Phase Sciences Corporation (SPSC) proposes to produce a library of heptapeptide analogs and a library of alkylether substituted pyrolidineanalide analogs targeting the delta and k (kappa) opioid receptors. Both compound libraries will consist of 2-5 milligrams each of a total of 192 compounds. SPSC will accomplish this by utilizing it's novel high-loading paramagnetic support and a commercially available solvent delivery robot. Specifically, libraries will be made off of this high-loading paramagnetic support, utilizing sonication to assist in the mixing and running of the reactions. A constant magnetic field will be used to separate the support from the soluble components of the reaction mixture. A liquid handling robot will be used to add reagents and solvents and to remove waste solvents through suction. The goal of the Phase I effort will be to integrate sonication, magnetic separation and automated liquid handling into one automated system to produce a library composed of peptide and non- peptide compounds for opioid receptor screening.