共查询到18条相似文献,搜索用时 171 毫秒
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外消旋体拆分是获取单一对映体药物的主要方法 ,将主 客化学引入化学拆分发明的包结拆分法突破了经典拆分方法的局限 ;酶法拆分目前用的最多的是水解和酯交换反应 ;模拟移动床色谱是商业规模制备色谱最有希望的技术 ;逆流萃取和膜分离技术是近年发展的分离对映体药物或中间体的更为经济的手性分离技术。不对称合成已走出实验室进入工业生产 ,常用的方法有手性源法、不对称催化法和生物转化法 相似文献
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不对称转换法制备D(-)-对羟基苯甘氨酸的研究 总被引:1,自引:0,他引:1
采用不对称转换法制备D( ) 对羟基苯甘氨酸(D( ) HPG)。DL(±) HPG在醋酸溶剂中,以甲苯磺酸(TS)为拆分剂,在苯甲醛的催化下制得D( ) HPG·TS盐,讨论了催化剂的用量、反应温度及反应时间对收率的影响,确定最佳工艺条件为:DL HPG∶TS∶苯甲醛=1∶1 025∶0 1(mol),反应温度100℃,反应时间6h。然后用氨水调pH至5~6得D( ) HPG。总收率为77 3%,光学纯度为98 9%。 相似文献
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L-脯氨酸在正丁醛或水杨醛催化作用下,可在羧酸中消旋。对L-脯氨酸在不同溶剂、温度、催化剂、反应时问下的消旋作了研究。采用不对称转换的方法,S-酒石酸作拆分剂,正丁醛作催化剂,正丁酸作溶剂,经过D-脯氨酸酒石酸盐,合成D-脯氨酸。在最佳工艺条件下的收率为92.4%,光学纯度为100%。 相似文献
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以L-甲硫氨酸为原料,3-溴-5-氯水杨醛为消旋催化剂,D-二对甲基苯甲酰酒石酸为拆分剂,在甲醇溶液中实现L-甲硫氨酸不对称转化制备得到D-甲硫氨酸,单程收率>80%,光学纯度>99%。 相似文献
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以L脯氨酸为原料、(2R,3R)酒石酸为拆分剂,采用不对称转换的方法将L-脯氨酸转换成D-脯氨酸。再以D-脯氨酸为原料,先后与乙酰氯、三乙胺和(BOC)2O反应,最后与苯基溴化镁反应,经乙酸乙酯萃取制得目标产物R-二苯基脯氨醇。总产率为46%。 相似文献
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4-氯-2-氨基苯酚重氮化后,分别与1-(4’-磺酸基)苯基-3-甲基-5-吡唑酮和1-苯基-3-甲基-5-吡唑酮偶合,得到偶氮物I和偶氮物Ⅱ;偶氮物I和氧化铬铬化反应得到络合物Ⅲ;络合物Ⅲ再与偶氮物Ⅱ在碱性条件下反应得到红色不对称金属络合染料(酸性红S—GN)。本文介绍了该染料的化学结构及合成方法。 相似文献
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Ferial M. Atta 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》1994,61(3):225-229
3-(2′-Chloroethyl)-2-methyl-3,4-dihydroquinazolin-4-one ( I ) was reacted with sodio (sodium thioglycolate) in dry dioxane and yielded compound II . By using thionyl chloride, this compound was converted to the corresponding acid chloride ( III ). The prepared acyl chloride ( III ) was allowed to interact with different α-amino acids such as Gly, L -Ala, L -B-Phe, DL -Asp, L -Glu, L -Thr and L -Val to give new amino acid derivatives ( IVa – g ). A selected C-terminal derivative of glycine ( IVa ) was converted into acid chloride ( V ). The acid chloride formed was reacted with L -Ala, L -B-Phe, DL -Asp, L -Glu, L -Thr and L -Val and yielded the new dipeptides VIa – f . The structures of the synthesized compounds were elucidated by elemental analysis and IR spectra. The prepared peptides were tested for their antimicrobial activities by comparison with tetra-cycline as a reference compound. 相似文献
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An electrochemical method was used to measure the mean activity coefficients of amino acids in water‐electrolyte‐amino acid systems. The amino acids were glycine, DL‐serine and DL‐valine and the electrolytes were KNO3 and NaNO3. The activity coefficients of the electrolytes were obtained from the e.m.f measurements in an electrochemical cell with an anion and a cation ion‐selective electrodes, each measured versus a double junction reference electrode at 298.15 K. The activity coefficients of the amino acids in the ternary systems were obtained from those of the electrolyte according to the cross differential relation. A simple semi‐empirical model based on a modification of a more complex form, derived from perturbation theory, was used to correlate the activity coefficients in binary aqueous solutions and in ternary systems. 相似文献
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Manuel Jrres Xia Chen Jos Luis Acea Carina Merkens Carsten Bolm Hong Liu Vadim A. Soloshonok 《Advanced Synthesis \u0026amp; Catalysis》2014,356(10):2203-2208
A new multipurpose glycine equivalent for the general asymmetric synthesis of α‐amino acids is introduced. The chiral reagent can be transformed to various amino acids by alkylations with alkyl halides as well as aldol and Michael addition reactions under operationally convenient reaction conditions at room temperature with virtually complete stereochemical control.
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在甲醇钠碱性条件下,以芦竹碱和N-乙酰氨基丙二酸二乙酯为原料进行缩合反应,缩合产物在4%的氢氧化钠水溶液中选择性水解脱羧得到N-乙酰-DL-色氨酸,然后在10%氢氧化钠水溶液中水解得到DL-色氨酸。DL-色氨酸用D-酒石酸拆分,并在苯甲醛催化下实现不对称转化,得到D-色氨酸D-酒石酸盐,最后用三乙胺中和得到目标产物D-色氨酸。确定了缩合和拆分步骤的适宜工艺条件。缩合步骤:甲醇钠摩尔量为芦竹碱的20%,n(芦竹碱)∶(N-乙酰氨基丙二酸二乙酯)=1∶1.2;拆分步骤:乙酸为溶剂,70℃反应,苯甲醛摩尔量为DL-色氨酸的10%,n(DL-色氨酸)∶n(D-酒石酸)=1∶2。 相似文献
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Nonproteinogenic α- or β-amino acids have attracted tremendous attention, as they are widely utilized for biological, biochemical, pharmaceutical, and asymmetric chemical investigations. Recently, we developed a series of new strategies for preparing achiral and chiral nickel(ii) complexes for the synthesis of amino acids. We applied these new methods utilizing chiral nickel(ii) complexes for the asymmetric Mannich reaction to synthesize enantiopure α,β-diamino acids, the enantioselective tandem conjugate addition-elimination reaction to prepare glutamic acid derivatives, the Suzuki coupling reaction to yield β(2)-amino acid derivatives, the asymmetric Mannich reaction to synthesize 3-aminoaspartate, the asymmetric Michael addition reaction to give β-substituted-α,γ-diaminobutyric acid derivatives, the asymmetric alkylation reaction to prepare linear ω-trifluoromethyl containing amino acids, and the asymmetric Michael addition reaction to synthesize syn-β-substituted tryptophans. 相似文献