共查询到19条相似文献,搜索用时 799 毫秒
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本文以樟脑衍生物(-)-莰烷磺内酰胺(2)为原料,经N-烷酰基莰烷-2,10-磺内酚胺(3)与碘代烷的不对称烷基化反应,用二锂代乙基苯基砜取代磺内酰胺助剂以及铝汞还原性脱硫反应等三步合成(S)和(R)一切叶蚁警戒信息素(1),其光学纯度高达95%e.e以上。 相似文献
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报道了(R)-和(S)-磷酸苯丙哌林对映体的合成新方法.以邻苄基苯酚和(S(+)-环氧氯丙烷为原料,通过成醚、选择性还原开环两步反应简捷高效地制得重要中间体(R)-1-(2-苄基苯氧基)-2-丙醇(2).中间体2与对甲苯磺酰氯酰化,制得中间体(R)-1-(2-苄基苯氧基)-2-丙醇对甲苯磺酸酯(3),该中间体与哌啶发生一次SN2反应直接得到(S)-(—)-苯丙哌林,该中间体与溴化锂和哌啶发生两次SN2反应制得(R)-(+)-苯丙哌林.然后它们分别与磷酸成盐制得相应的(S)-(—)-和(R)-(+)-磷酸苯丙哌林,其结构通过1H NMR和HRMS进行了表征.该合成方法路线短,反应条件温和,易于操作,且收率好,适合工业化生产. 相似文献
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手性γ-孟氧基丁烯酸交酯在构成各种杂环化合牧天然产物中起重要作用.本文报道了一些新的γ-孟氧基丁烯交酯的新的手性源的制备和研究了它们的不对称反应. 相似文献
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N-Methyl-N-[(1S)-1-[(3R)-pyrrolidin-3-yl]ethyl]amine (1)(1) is a key intermediate in the preparation of premafloxacin (2), which was under development as an antibiotic for use against pathogens of veterinary importance. This paper describes the development of a practical, efficient, and stereoselective process for the preparation of 1 from isobutyl (3S)-3-[methyl[(1S)-1-phenylethyl]amino]butanoate (5c). The key steps in the synthetic sequence are an asymmetric Michael addition, which yields 5c, and a stereoselective alkylation, which yields (3S,4S)-3-allyl-1,4-dimethylazetidin-2-one (17). 相似文献
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(1'R,3R,4R)-N-取代-3-(1'-羟基乙基)-4-乙酰氧基-β-内酰胺(3)是合成青霉烯和碳青霉烯类β-内酰胺抗生素的关键中间体。以廉价的L-抗坏血酸为原料,制得S-缩异丙氧叉甘油醛(5),与胺反应定量转变成相应的手性亚胺(6a~6d),6与双烯酮[2+2]环加成反应,高立体选择性地合成3(S)-乙酰基-β-内酰胺(8a~8d),其非对映体过量由类似反庆的80%提高到接近100%。8a经四步反应得到目标化合物3a。 相似文献
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[reaction:see text] During the total synthesis of the novel cyclic depsipeptide callipeltin A (1), the unit (3S,4R)-3,4-dimethylglutamine, was successfully synthesized by asymmetric Michael addition and subsequent electrophilic azidation. The key feature of this approach is the generation of three adjacent stereogenic centers using the same camphorsultam chiral auxiliary. 相似文献
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An efficient enantioselective total synthesis of (R)-rolipram and an efficient enantioselective formal synthesis of (3S,4R)-paroxetine has been achieved using the highly enantioselective Michael addition of malonate nucleophiles as key steps in both cases. 相似文献
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Revial G Lim S Viossat B Lemoine P Tomas A Duprat AF Pfau M 《The Journal of organic chemistry》2000,65(15):4593-4600
The Michael reaction of chiral 3-substituted secondary enaminoesters with 2-substituted nitroethylenes leads to (Z)-adducts, with good to excellent diastereoselectivity. The nitro group of these adducts was catalytically reduced to give, after cyclization and chiral amine elimination, pyrrolines or pyrrolidines after further reduction. In particular, the syntheses of ethyl (2R,3S,4S)-2,4-dimethylpyrrolidine-3-carboxylate and ethyl (2R,3R,4S)-2-(4-methoxyphenyl)-4-(3,4-(methylenedioxy)phenyl)pyrrolidine-3-carboxylate are described. 相似文献
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The stereoselective synthesis of (2R,4R)-2-N-tert-butyloxycarbonyl amino-4,5-epoxido-valeric acid methyl ester 8,which is the key intermediate for the synthesis of (2′S,2R)-3-trans-nitrocyclopropyl-alanine,was first accomplished. 相似文献
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The nonproteinogenic amino acids (3S,4R)-3,4-Dimethyl-l-pyroglutamic acid and (3S,4R)-3,4-dimethyl-l-glutamine -- found in the cyclic depsipeptides callipeltin B, callipeltin A, and papuamide A -- were synthesized from a common intermediate derived from l-pyroglutamic acid. The diastereoselective introduction of the methyl groups was accomplished by cuprate addition and enolate alkylation, followed by a kinetic epimerization of the C-4 methyl substituent. (3S,4R)-3,4-dimethyl-l-glutamine shows a conformational restriction of its side chain which may be related to its biological function in the natural products where it is found. 相似文献