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3,4 (6 karubokishimetano) proline

机译:3,4(压缩了6个轻如歌舞)p Roine

摘要

PURPOSE: To obtain the new compound consisting of 3,4-(6-carboxymethano) proline, having suppressing action against L-glutamic acid transporter's intake activity on a glutamic acid of a neurotransmitter and useful for the treatment of a neuron degenerative disease. ;CONSTITUTION: This is a new compound of a 3,4-(6-carboxymethano)proline [e.g. (2S,3S,4S,6R)-3,4-(6-carboxymethano)prolinel which has a suppressive action against the intake activity of a neurotransmitter, i.e., an L-glutamic acid expressed by formula I, useful for the elucidation of the function of a glutamic acid transporter and expected to develop in the field of e.g. treatment of a neuron degenerative disease, e.g. epilepsy, Huntington's chorea and Parkinson's disease. This compound is obtained by opening the oxazolidine ring of a compound of formula II (TBS is t-butyldimethylsilyl), protecting the hydroxyl and amino groups, then reducing the product to obtain a compound of formula III (Boc is t-butoxycarbonyl), removing protecting groups (TBS), subjecting the product to Jones oxidation and then methyl esterification, hydrolyzing and finally removing the protecting group (Boc) successively.;COPYRIGHT: (C)1995,JPO
机译:目的:获得由3,4-(6-羧甲基)脯氨酸组成的新化合物,该化合物具有抑制L-谷氨酸转运蛋白对神经递质谷氨酸的摄取活性的作用,可用于治疗神经元变性疾病。 ;组成:这是3,4-(6-羧甲基)脯氨酸的新化合物[例如(2S,3S,4S,6R)-3,4-(6-羧甲基)脯氨酸对神经递质的摄取活性具有抑制作用,即由式I表示的L-谷氨酸,可用于阐明谷氨酸转运蛋白的功能,并有望在例如神经元退行性疾病的治疗,例如癫痫,亨廷顿舞蹈病和帕金森氏病。通过打开式Ⅱ化合物(TBS为叔丁基二甲基甲硅烷基)的恶唑烷环,保护羟基和氨基,然后还原产物以获得式Ⅲ化合物(Boc为叔丁氧羰基),除去保护基团(TBS),使产物经受琼斯氧化,然后进行甲基酯化,水解,最后依次除去保护基团(Boc)。;版权:(C)1995,JPO

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