180587-74-0Relevant academic research and scientific papers
Preparation method for tenofovir
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Paragraph 0065-0071; 0072-0079, (2018/07/30)
The invention relates to the field of chemical synthesis, and in particular relates to a preparation method for tenofovir. The compound provided by the invention has a structure shown by a formula XIIin the description. The method for preparing the tenofovir based on a compound provided by the invention has the advantages that raw materials are cheap and easy to obtain, the process route is short, the conditions are mild and reliable, and the method is easily used for industrialized production.
(R)- (+) - 9 - (2 - hydroxypropyl) adenine preparation method
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Paragraph 0040, (2017/07/01)
The invention discloses a preparation method of (R)-(+)-9-(2-hydroxypropyl) adenine, which is a key intermediate for tenofovir disoproxil fumarate. The method comprises the following steps: (1) reacting 6-chloropurine and bromopropanone to obtain 6-chloro-9-(acetonyl)-purine; (2) performing an asymmetric hydrogenation reduction reaction of the resultant 6-chloro-9-(acetonyl)-purine to obtain (R)-(+)-6-chloro-9-(2-hydroxypropyl) adenine; and (3) performing an aminolysis reaction of the resultant (R)-(+)-6-chloro-9-(2-hydroxypropyl) adenine to obtain (R)-(+)-9-(2-hydroxypropyl) adenine. An achiral compound, cheap and easy to obtain, is taken as a raw material in the method; the reaction steps are small; the reaction is easy to deal with; the enantioselectivity of the product is high; and the yield is high, and thus the preparation method has industrialization value.
The synthesis of tenofovir and its analogues via asymmetric transfer hydrogenation
Zhang, Qian,Ma, Bai-Wei,Wang, Qian-Qian,Wang, Xing-Xing,Hu, Xia,Xie, Ming-Sheng,Qu, Gui-Rong,Guo, Hai-Ming
supporting information, p. 2014 - 2017 (2014/05/06)
A series of tenofovir analogues with potential antiviral and immunobiologically active compounds were synthesized through an asymmetric transfer hydrogenation reaction from achiral purine derivatives. Up to 97% ee and good to excellent yields were achieved under mild conditions through short reaction steps. The present report suggests an efficient process to acquire tenofovir and its analogues.
