imino ester
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It was found that the more easily systhesized and stable N, N-acetal or N, Ohemiacetal can replace N-tosyl imino ester to react with phenols in the presence of TiCl〓, and α-arylglycine derivatives were also obtained in high yields and high regioselectivity.
进一步研究发现,更易合成的N,N-或N,O-缩醛可以作为亚胺酯的替代物和酚类化合物发生傅克反应。路易酸TiCl〓能有效地促进酚类化合物和亚胺酯的傅克反应较高产率、较高区域选择性的得到2-羟基α-芳香甘氨酸衍生物。
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In the forth part, in the presence of chiral phosphoric acid, highly enantio-enriched (up to 98% ee)α-aryl glycine derivatives could be synthesized via asymmetric transfer hydrogenation of the α-aryl imino esters using Hantzsch ester as the hydrogen source.
第四部分工作中,利用Hantzsch酯作为氢源,高对映选择性地实现了手性磷酸催化芳基酮酸酯亚胺的不对称仿生氢化反应,以最高98%的对映选择性得到苯甘氨酸衍生物。
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A type of novel dis-substituted α-arylglycine derivatives was synthesized in high yields and high regioselectivity via the stepwise Friedel-Crafts reaction of phenols with N-tosyl imino ester promoted by TiCl〓.
发现在Mg/MeOH/超声波条件下,能高产率的得到N-Tos裂解后N-Boc保护的α-芳香甘氨酸衍生物,实现了一条简单、实用的合成N-Boc保护的α-芳香甘氨酸衍生物的方法。
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The novel synthesis of the 2-hydroxyl α-arylglycines was realized through the Lewis acids promoted Friedel-Crafts reaction of phenols and N-tosyl imino ester in mild reaction conditions.
其中在路易酸TiCl〓促进下,酚类化合物和亚胺酯发生的傅克反应,可较高产率、较高区域选择性的得到2-羟基α-芳香甘氨酸衍生物。
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In the fifth part, asymmetric synthesis of β,γ-trans-alkenyl α-amino esters was achieved by chiral phosphoric acid catalyzed transfer hydrogenation of β,γ-alkynyl α-imino esters. Utilizing Hantzsch ester as the hydrogen donor, both the alkyne and imine moieties of β,γ-alkynyl α-imino esters were reduced to yield β,γ-trans-alkenyl α-amino esters with up to 96% ee.
第五部分工作中,使用手性磷酸作为催化剂,Hantzsch酯作为氢源,β,γ-炔烃取代的α-酮酸酯亚胺中的炔键和亚胺官能团均被还原,以中等的收率和优秀的对映选择性(up to 96% ee)得到β,γ-反式烯烃取代的α-氨基酸衍生物。
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imino acid ester:亚胺醚;亚胺酸酯
imino ether 亚胺醚;亚胺酸酯 | imino acid ester 亚胺醚;亚胺酸酯 | imine 亚胺