- Preparation method and application of (3R, 4S)-4-ethylpyrrolidine-3-carboxylic acid compound
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The embodiment of the invention discloses a preparation method and application of a (3R, 4S)-4-ethylpyrrolidine-3-carboxylic acid compound, and relates to the technical field of drug synthesis. The (3R, 4S)-4-ethylpyrrolidine-3-carboxylic acid is synthesized by taking glycine ethyl ester as a raw material and sequentially carrying out amino protecting group addition, ring closing, substitution, coupling, catalytic hydrogenation, hydrolysis and protecting group removal. The target product synthesized by the reaction has high yield and chiral purity, and also has the advantages of simple and accessible raw materials, simple synthesis route, mild reaction conditions, simple separation and purification operation and low synthesis cost.
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Paragraph 0047-0050
(2020/05/14)
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- Palladium-catalysed enantioselective α-hydroxylation of β-ketoesters
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Highly enantioselective α-hydroxylation of cyclic and acyclic 1,3-ketoesters can be achieved with up to 98% ee using a dicationic palladium(ii) catalyst and dimethyldioxirane as oxidant.
- Smith, Alexander M.R.,Billen, Denis,Hii, King Kuok
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supporting information; experimental part
p. 3925 - 3927
(2010/01/06)
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- New facile alkoxycarbonylating agent, alkyl pyrazole-1-carboxylates. The preparation and the utilities
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Alkyl pyrazole-1-carboxylates (2), which were readily prepared from alkyl chloroformate or carbazate in good yields, were provided as the new facile alkoxycarbonylating agents toward the Grignard reagents for the synthesis of one carbon higher carboxylic esters. Also amines were alkoxycarbonylated by 2 to produce the corresponding urethanes even in an aqueous medium. Benzyl 3,5-dimethylpyrazole-1-carboxylate (2d) could be utilized for the Cbz-protection of amino acids and esters in good yield without any racemization.
- Kashima, Choji,Tsuruoka, Shiro,Mizuhara, Saori
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p. 14679 - 14688
(2007/10/03)
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- Preparation of 3-pyrrolidone and 4-perhydroazepinone
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Efficient multigram preparations of 3-pyrrolidone by sequential Michael addition and Dieckmann condensation, and of 4-perhydroazepinone by ring expansion have been achieved.
- Roglans,Marquet,Moreno-Manas
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p. 1249 - 1258
(2007/10/02)
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- Process for preparing phosphonomethylated amino acids
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A process for preparing phosphonomethylated amino acids comprising phosphonomethylating an N-carbamylated amino acid derivative with formaldehyde and a phosphorus source to obtain a phosphonomethylated N-carbamylated amino acid derivative which is then hydrolyzed to the corresponding phosphonomethylated amino acid, e.g. glyphosate, or acid derivative.
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