- Preparation Method of Nucleoside Phosphoramidate Prodrugs and Intermediates Thereof
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Provided in the present disclosure are a novel preparation method of nucleoside phosphoramidate prodrugs and the intermediates thereof. In particular, the method is adopted to perform isomer separation on the reaction product from a first step and then perform a two-step chemical synthesis, so as to prepare a high-purity compound Sp-1. The method has simple and convenient operation and low cost. The prepared resulting single isomer Sp-1 has high purity, and the HPLC purity thereof is 95% or more, and further, 99% or more. The method is suitable for industrial production and can satisfy the need of clinical study. Further, also provided in the present disclosure are a key intermediate phosphorus reagent for preparing the high-purity compound Sp-1 and the preparation method thereof.
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Paragraph 0131; 0132
(2018/09/12)
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- STEREOSELECTIVE SYNTHESIS OF BETA-NUCLEOSIDES
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A process of stereoselectively synthesizing β-nucleoside of formula (I), e.g., 2'-deoxy-2,2'-difluorocytidine, is described. The process includes reacting a tetrahydrofuran compound of the following formula: in which wherein R1, R2, R3, R4, and L as defined in the specification, with a nucleobase derivative in the presence of an oxidizing agent.
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Page/Page column 12
(2012/10/18)
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