The Experts below are selected from a list of 906 Experts worldwide ranked by ideXlab platform
Hong Liu - One of the best experts on this subject based on the ideXlab platform.
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gold i catalyzed cascade approach for the synthesis of tryptamine based polycyclic privileged scaffolds as α1 adrenergic receptor antagonists
Journal of Organic Chemistry, 2013Co-Authors: Nan Yang, Ying Chen, Yu Zhou, Lei Zhang, Jinfang Wang, Xin Xie, Hong LiuAbstract:An efficient and facile gold(I)-catalyzed one-pot cascade protocol has been developed for the synthesis of tryptamine-fused polycyclic privileged structures through the treatment of substituted Tryptamines and 2-ethynylbenzoic acids or 2-ethynylphenylacetic acids. This strategy features the formation of one C–C bond and two C–N bonds with high yields and broad substrate tolerance. The selected reduced target molecules are validated to perform as α1-adrenergic receptors antagonists. The most potent one, 4bh, exhibits an IC50 value of 277 nM on α1A subtype with a selectivity ratio of 15.8 over α1B subtype.
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Gold(I)-Catalyzed Cascade Approach for the Synthesis of Tryptamine-Based Polycyclic Privileged Scaffolds as α1‑Adrenergic Receptor Antagonists
2013Co-Authors: Nan Yang, Ying Chen, Yu Zhou, Lei Zhang, Jinfang Wang, Xin Xie, Hong LiuAbstract:An efficient and facile gold(I)-catalyzed one-pot cascade protocol has been developed for the synthesis of tryptamine-fused polycyclic privileged structures through the treatment of substituted Tryptamines and 2-ethynylbenzoic acids or 2-ethynylphenylacetic acids. This strategy features the formation of one C–C bond and two C–N bonds with high yields and broad substrate tolerance. The selected reduced target molecules are validated to perform as α1-adrenergic receptors antagonists. The most potent one, 4bh, exhibits an IC50 value of 277 nM on α1A subtype with a selectivity ratio of 15.8 over α1B subtype
Nan Yang - One of the best experts on this subject based on the ideXlab platform.
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gold i catalyzed cascade approach for the synthesis of tryptamine based polycyclic privileged scaffolds as α1 adrenergic receptor antagonists
Journal of Organic Chemistry, 2013Co-Authors: Nan Yang, Ying Chen, Yu Zhou, Lei Zhang, Jinfang Wang, Xin Xie, Hong LiuAbstract:An efficient and facile gold(I)-catalyzed one-pot cascade protocol has been developed for the synthesis of tryptamine-fused polycyclic privileged structures through the treatment of substituted Tryptamines and 2-ethynylbenzoic acids or 2-ethynylphenylacetic acids. This strategy features the formation of one C–C bond and two C–N bonds with high yields and broad substrate tolerance. The selected reduced target molecules are validated to perform as α1-adrenergic receptors antagonists. The most potent one, 4bh, exhibits an IC50 value of 277 nM on α1A subtype with a selectivity ratio of 15.8 over α1B subtype.
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Gold(I)-Catalyzed Cascade Approach for the Synthesis of Tryptamine-Based Polycyclic Privileged Scaffolds as α1‑Adrenergic Receptor Antagonists
2013Co-Authors: Nan Yang, Ying Chen, Yu Zhou, Lei Zhang, Jinfang Wang, Xin Xie, Hong LiuAbstract:An efficient and facile gold(I)-catalyzed one-pot cascade protocol has been developed for the synthesis of tryptamine-fused polycyclic privileged structures through the treatment of substituted Tryptamines and 2-ethynylbenzoic acids or 2-ethynylphenylacetic acids. This strategy features the formation of one C–C bond and two C–N bonds with high yields and broad substrate tolerance. The selected reduced target molecules are validated to perform as α1-adrenergic receptors antagonists. The most potent one, 4bh, exhibits an IC50 value of 277 nM on α1A subtype with a selectivity ratio of 15.8 over α1B subtype
Yury V Tomilov - One of the best experts on this subject based on the ideXlab platform.
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synthesis of branched Tryptamines via the domino cloke stevens grandberg rearrangement
Journal of Organic Chemistry, 2017Co-Authors: Rinat F Salikov, Konstantin P Trainov, Anastasia A Levina, Irina K Belousova, Michael G Medvedev, Yury V TomilovAbstract:The rearrangement of cyclopropylketone arylhydrazones generated in situ from arylhydrazine hydrochlorides and ketones leads to formation of tryptamine derivatives. The use of (2-arylcyclopropyl)ethanones in the reactions with model 4-bromophenylhydrazine hydrochloride gives branched Tryptamines with aryl groups in the α-position to the amino group, while (2-methylcyclopropyl)ethanone gives a mixture of α- and β-substituted products in a ratio of 1:3. The method was found effective in the synthesis of enantiomerically pure tryptamine. Thus, (R,R)-(2-phenylcyclopropyl)ethanone gives the (S)-α-phenyltryptamine derivative with an enantiomeric excess over 99%.
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Synthesis of Branched Tryptamines via the Domino Cloke–Stevens/Grandberg Rearrangement
2016Co-Authors: Rinat F Salikov, Konstantin P Trainov, Anastasia A Levina, Irina K Belousova, Michael G Medvedev, Yury V TomilovAbstract:The rearrangement of cyclopropylketone arylhydrazones generated in situ from arylhydrazine hydrochlorides and ketones leads to formation of tryptamine derivatives. The use of (2-arylcyclopropyl)ethanones in the reactions with model 4-bromophenylhydrazine hydrochloride gives branched Tryptamines with aryl groups in the α-position to the amino group, while (2-methylcyclopropyl)ethanone gives a mixture of α- and β-substituted products in a ratio of 1:3. The method was found effective in the synthesis of enantiomerically pure tryptamine. Thus, (R,R)-(2-phenylcyclopropyl)ethanone gives the (S)-α-phenyltryptamine derivative with an enantiomeric excess over 99%
Shuli You - One of the best experts on this subject based on the ideXlab platform.
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chiral amine catalyzed asymmetric bromocyclization of tryptamine derivatives
Asian Journal of Organic Chemistry, 2014Co-Authors: Quan Cai, Qin Yin, Shuli YouAbstract:Chiral hexahydropyrro[2,3]indole (HPI) units exist widely in natural and unnatural products with significant biological activities. The enantioselective synthesis of brominated hexahydropyrrolo[2,3-b]indole (HPI) subunits by asymmetric bromocyclization of tryptamine derivatives catalyzed by a chiral amine has been realized. In the presence of hydroquinine 1,4-phthalazinediyl diether ((DHQ)2PHAL, 20 mol %) and L-(-)-camphorsulfonic acid (20 mol %), enantioenriched brominated HPI derivatives were obtained from readily available substituted Tryptamines in up to 99% yield and 73% ee.
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enantioselective construction of pyrroloindolines via chiral phosphoric acid catalyzed cascade michael addition cyclization of Tryptamines
Organic Letters, 2012Co-Authors: Quan Cai, Chuan Liu, Xiaowei Liang, Shuli YouAbstract:Enantioselective construction of pyrroloindolines via chiral phosphoric acid catalyzed cascade Michael addition–cyclization of Tryptamines has been realized. With 5 mol % of chiral phosphoric acid, enantioenriched pyrroloindoline derivatives were obtained in good yields and enantioselectivity (up to 95% yield and 83% ee) from readily available Tryptamines and enones.
Yu Zhou - One of the best experts on this subject based on the ideXlab platform.
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gold i catalyzed cascade approach for the synthesis of tryptamine based polycyclic privileged scaffolds as α1 adrenergic receptor antagonists
Journal of Organic Chemistry, 2013Co-Authors: Nan Yang, Ying Chen, Yu Zhou, Lei Zhang, Jinfang Wang, Xin Xie, Hong LiuAbstract:An efficient and facile gold(I)-catalyzed one-pot cascade protocol has been developed for the synthesis of tryptamine-fused polycyclic privileged structures through the treatment of substituted Tryptamines and 2-ethynylbenzoic acids or 2-ethynylphenylacetic acids. This strategy features the formation of one C–C bond and two C–N bonds with high yields and broad substrate tolerance. The selected reduced target molecules are validated to perform as α1-adrenergic receptors antagonists. The most potent one, 4bh, exhibits an IC50 value of 277 nM on α1A subtype with a selectivity ratio of 15.8 over α1B subtype.
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Gold(I)-Catalyzed Cascade Approach for the Synthesis of Tryptamine-Based Polycyclic Privileged Scaffolds as α1‑Adrenergic Receptor Antagonists
2013Co-Authors: Nan Yang, Ying Chen, Yu Zhou, Lei Zhang, Jinfang Wang, Xin Xie, Hong LiuAbstract:An efficient and facile gold(I)-catalyzed one-pot cascade protocol has been developed for the synthesis of tryptamine-fused polycyclic privileged structures through the treatment of substituted Tryptamines and 2-ethynylbenzoic acids or 2-ethynylphenylacetic acids. This strategy features the formation of one C–C bond and two C–N bonds with high yields and broad substrate tolerance. The selected reduced target molecules are validated to perform as α1-adrenergic receptors antagonists. The most potent one, 4bh, exhibits an IC50 value of 277 nM on α1A subtype with a selectivity ratio of 15.8 over α1B subtype
