- Copper-Catalyzed Asymmetric Hydrosilylation of β-Nitroethyl Aryl Ketones
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A copper-catalyzed asymmetric hydrosilylation of β-nitroethyl aryl ketones has been disclosed, and the corresponding chiral alcohols could be obtained in high yields (up to 99% yield) and excellent enantioselectivities (up to 96% ee). Moreover, the reaction worked well on a gram scale with 0.3 mol % of ligand loading, indicating that our protocol has potential applications in the synthesis of important pharmaceuticals such as Tranylcypromine and Ticagrelor.
- Zeng, Weijun,Tan, Xuefeng,Yu, Yang,Chen, Gen-Qiang,Zhang, Xumu
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p. 858 - 862
(2020/01/31)
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- Highly enantioselective bioreduction of 1-(3,4-difluorophenyl)-3-nitropropan-1-one: Key intermediate of ticagrelor
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A simple, highly effective and economical whole-cell mediated process was developed for the biocatalytic reduction of a ketone, intermediate in the synthesis of platelet inhibiting drug ticagrelor. Sixteen different microorganisms were screened for the bi
- Singh, Manpreet,Krishnen, Hare,Neelam, Uday Kumar,Charugondla, Kavitha,Gilla, Goverdhan,Holt-Tiffin, Karen,Bandichhor, Rakeshwar
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p. 35086 - 35090
(2016/05/19)
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- Biocatalytic approaches to a key building block for the anti-thrombotic agent ticagrelor
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Three complementary biocatalytic routes were examined for the synthesis of the cyclopropyl amine (1R,2S)-2, which is a key building block for the anti-thrombotic agent ticagrelor 1. By employing either a ketoreductase, amidase or lipase biocatalyst, the k
- Hugentobler, Katharina G.,Sharif, Humera,Rasparini, Marcello,Heath, Rachel S.,Turner, Nicholas J.
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supporting information
p. 8064 - 8067
(2016/09/09)
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- Synthesis of nitrogen substituted cyclopropanes
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The invention is about a new synthetic pathway for the preparation of enantiomerically pure nitrogen substituted cyclopropanes, in particular the trans-cyclopropanamine (1), a key intermediate in the synthesis of Ticagrelor: The invention also relates to
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Paragraph 0147-0148
(2013/05/22)
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- NOVEL PROCESS FOR PREPARING PHENYLCYCLOPROPYLAMINE DERIVATIVES USING NOVEL INTERMEDIATES
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Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.
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Paragraph 0147
(2013/06/27)
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- NOVEL PROCESSES FOR PREPARING TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF
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Provided herein is a novel process for the preparation of triazolo[4,5-d]pyrimidine derivatives. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of highly pure ticagrelor or a pharmaceutically acceptable salt thereof. Provided further herein is a novel process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d] [1,3]- dioxol-4-yl]oxy]- 1 -ethanol.
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Page/Page column 47-48
(2012/07/13)
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- NOVEL PROCESS FOR PREPARING PHENYLCYCLOPROPYLAMINE DERIVATIVES USING NOVEL INTERMEDIATES
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Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.
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Page/Page column 33-34
(2011/11/06)
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