1383959-11-2Relevant articles and documents
Substituted n-pentanamide compounds, preparation method and the use thereof
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Paragraph 0150-0151, (2014/03/21)
The present invention relates to a (2R, 3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process.
SUBSTITUTED N-PENTANAMIDE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
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Paragraph 0132; 0133, (2014/01/08)
The present invention relates to a (2R, 3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process.
A practical and enantioselective synthesis of tapentadol
Zhang, Qiang,Li, Jian-Feng,Tian, Guang-Hui,Zhang, Rong-Xia,Sun, Jin,Suo, Jin,Feng, Xin,Fang, Du,Jiang, Xiang-Rui,Shen, Jing-Shan
experimental part, p. 577 - 582 (2012/08/27)
A practical and enantioselective synthetic method for tapentadol has been described. Starting from inexpensive and readily available (E)-3-(3-(benzyloxy) phenyl)acrylic acid, tapentadol was prepared in seven steps (44% overall yield and 99.9% de) in more than 100 g batches, without any chromatographic purification. An Evans' chiral auxiliary based conjugate addition and alkylation were used as the key steps.