1088705-53-6Relevant articles and documents
Novel synthesis method of oseltamivir
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Paragraph 0104-0108, (2021/05/19)
The invention provides a novel synthesis method of oseltamivir. The synthesis method comprises the following steps: taking a compound (E)-2-(2-nitrovinyl) isoindoline-1,3-diketone and ethyl pyruvate as initial raw materials, and carrying out Michael addition reaction under the condition of catalysis of a thiourea catalyst to obtain a corresponding Michael addition product; then, subjecting the Michael addition product and (formyl methylene) triphenyl phosphine to a Wittig reaction and a Henry reaction in a pot so as to obtain a ring closing product; and forming an etherified product from the ring closing product and a trichloroacetonitrile intermediate, and performing reduction, acetylation and de-protection to obtain oseltamivir. The reaction route comprises six steps, raw materials used in each step of reaction are easy to obtain and not expensive, the operation is easy, the yield of each step of reaction is high, no heavy metal or azide is used in the whole synthesis process, and the method is green and safe and can be applied to industrial production.
A highly efficient asymmetric Michael addition of α,α- disubstituted aldehydes to maleimides catalyzed by primary amine thiourea salt
Yu, Feng,Jin, Zhichao,Huang, Huicai,Ye, Tingting,Liang, Xinmiao,Ye, Jinxing
experimental part, p. 4767 - 4774 (2010/11/20)
The first highly efficient Michael addition of challenging α,α-disubstituted aldehydes to maleimides catalyzed by a simple bifunctional primary amine thiourea catalyst/benzoic acid system has been successfully developed to generate quaternary carbon cente
Highly effective and enantioselective α-amination of aldehydes promoted by chiral proline amide-thiourea bifunctional catalysts
Fu, Ji-Ya,Huang, Qing-Chun,Wang, Qiao-Wei,Wang, Li-Xin,Xu, Xiao-Ying
experimental part, p. 4870 - 4873 (2010/10/02)
A series of secondary amine-thiourea catalysts derived from l-proline and chiral diamine were prepared and first applied to highly enantioselective amination of unmodified aldehydes with various azodicarboxylates in excellent yields (up to 99%) and enanti