An improved asymmetric synthetic route to a novel triple uptake inhibitor antidepressant (2S,4R,5R)-2-benzhydryl-5-((4-methoxybenzyl)amino)tetrahydro-2H-pyran-4-ol (D-142) [0.03%]
一种新型三重再摄取抑制剂抗抑郁药物(D-142)的改进不对称合成路线研究
Bhaskar Gopishetty,Sanjib Gogoi,Aloke Dutta
Bhaskar Gopishetty
Triple monoamine reuptake inhibitors have been implicated in the development of a new generation of antidepressants with higher efficacy than the currently existing therapies. In this paper, we have developed an alternative efficient synthe...
Organocatalytic enantioselective tandem aldol-cyclization reaction of α-isothiocyanato imides and activated carbonyl compounds [0.03%]
α-异硫氰基亚胺和活化羰基化合物的有机催化串联aldol环化反应
Jie Guang,Cong-Gui Zhao
Jie Guang
The organocatalytic enantioselective tandem aldol-cyclization reactions of α-isothiocyanato imides and activated carbonyl compounds, such as isatins, an α-ketolactone and a 1,2-dione, have been studied with cinchona alkaloid-derived thiou...
Efficient, scalable asymmetric synthesis of an epoxy quinol via Noyori desymmetrization of a meso diketone [0.03%]
高效、可放大的通过Noyori动力学拆分内消旋二酮合成环氧喹诺里𬭩盐的方法
David R Clay,Ashley G Rosenberg,Matthias C McIntosh
David R Clay
Epoxy quinol 1a was prepared on a multi-gram scale by Noyori transfer hydrogenative desymmetrization of the readily available meso epoxy diketone 4. Although the intrinsic enantioselectivity for the desymmetrization was modest (82:18 er at ...
Spiroborate esters in the borane-mediated asymmetric synthesis of pyridyl and related heterocyclic alcohols [0.03%]
用于吡啶基和相关杂环醇的硼烷介导的手性合成中的旋伞花酯类物质研究
Viatcheslav Stepanenko,Melvin De Jesús,Wildeliz Correa et al.
Viatcheslav Stepanenko et al.
The effectiveness of several spiroborate ester catalysts was investigated in the asymmetric borane reduction of 2-, 3-, 4-acetylpyridines under different reaction conditions. Highly enantiomerically enriched 1-(2-, 3- and 4-pyridyl)ethanols...
Recent Progress on the Stereoselective Synthesis of Cyclic Quaternary alpha-Amino Acids [0.03%]
cyclic quaternary α-氨基酸立体选择性合成研究的新进展
Carlos Cativiela,Mario Ordóñez
Carlos Cativiela
The most recent papers describing the stereoselective synthesis of cyclic quaternary alpha-amino acids are collected in this review. The diverse synthetic approaches are classified according to the size of the ring and taking into account t...
Enantioselective organocatalytic alpha-sulfenylation of substituted diketopiperazines [0.03%]
光学活性有机小分子催化二酮哌嗪的α-磺烯化反应研究
Nathan W Polaske,Ramin Dubey,Gary S Nichol et al.
Nathan W Polaske et al.
The asymmetric organocatalytic alpha-sulfenylation of substituted piperazine-2,5-diones is reported, with cinchona alkaloids as chiral Lewis bases and electrophilic sulfur transfer reagents. Catalyst loadings, the type of sulfur transfer re...
Chiral spiroaminoborate ester as a highly enantioselective and efficient catalyst for the borane reduction of furyl, thiophene, chroman and thiochroman containing ketones [0.03%]
用于呋喃、噻吩、查尔曼和噻咯烷酮的硼氢化反应的手性螺氨基硼酸酯的高度对映选择性和高效催化剂
Viatcheslav Stepanenko,Melvin De Jesús,Wildeliz Correa et al.
Viatcheslav Stepanenko et al.
Prochiral heteroaryl ketones containing furan, thiophene, chroman and thiochroman moieties were successfully reduced in the presence of 1 - 10 mol % of spiroaminoborate ester 1 with different borane sources to afford non-racemic alcohols in...
Efficient alcoholysis of 5,6-dihydro-1,10-phenanthroline-5,6-epoxide with ytterbium(III) triflate and subsequent enantioselective transesterification with lipases [0.03%]
三氟甲磺酸镱催化5,6-二氢-1,10-菲并硫唑-5,6-环氧化合物的高效醇解反应及酯酶催化的动力学拆分反应
Elke Schoffers,Lars Kohler
Elke Schoffers
New 5,6-dihydro-1,10-phenanthroline derivatives were prepared in high yield via ytterbium(III) triflate-catalyzed alcoholysis of the corresponding epoxide. Enzymatic transesterifications of racemic alkoxy alcohols afforded enantioselective ...
Efficient access to enantiomerically pure cyclic alpha-amino esters through a lipase-catalyzed kinetic resolution [0.03%]
高效获得消旋环状α-氨基酸酯类化合物的动力学拆分法
Sergio Alatorre-Santamaría,María Rodriguez-Mata,Vicente Gotor-Fernández et al.
Sergio Alatorre-Santamaría et al.
A series of alpha-amino acid derivatives containing the 2,3-dihydroindole or octahydroindole core have been chemoenzymatically synthesized in good overall yields and high enantiomeric purity under mild reaction conditions using lipases for ...
Towards the stereoselective synthesis of alpha-methylated (2S,3aS,7aS)-octahydroindole-2-carboxylic acid [0.03%]
α-甲基化(2S,3aS,7aS)-辛氢吲哚-2-甲酸的立体选择性合成研究
Francisco J Sayago,M Isabel Calaza,Ana I Jiménez et al.
Francisco J Sayago et al.
A high yielding and remarkably stereoselective alpha-methylation reaction of the (2S,3aS,7aS) stereoisomer of octahydroindole-2-carboxylic acid, (S,S,S)-Oic, suitably protected is described. The severe steric hindrance imposed by the fused ...