1292296-09-3Relevant articles and documents
A facile and efficient synthesis of d3-labelled Reyataz
Zhang, Huiping,Bonacorsi Jr., Samuel J.,Chen, Bang-Chi,Leith, Leslie W.,Rinehart, J. Kent,Balasubramanian, Balu,Barrish, Joel C.
, p. 1041 - 1047 (2005)
A facile and efficient synthesis of d3-labelled Reyataz is described. The key step of synthesis involved the coupling of N-(d 3-methoxycarbonyl)-L-tert-leucine 2b with an advanced chiral non-racemic building block 4. The latter was synthesized in 4 steps from the readily accessible hydrazine derivative 8. Copyright
Method for synthesis of atazanavir
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, (2018/04/01)
The invention discloses a method for synthesis of atazanavir. The method comprises that a compound methyl (S)-1-((S)-2-ethoxyethyl-1-phenylethane-2-yl-amino)-3, 3-dimethyl-1-carbonylbutane-2-yl-carbamate shown in the formula V and a compound N-1-[N-(methoxycarbonyl)-L-tertiary leucine]-N-2-[4-(2-pyridyl)-benzyl]hydrazine shown in the formula VIII undergo a nucleophilic substitution reaction in anorganic solvent to produce a compound 1-[4-(2-pyridyl)phenyl]-5(S)-2, 5-bis{[N-(methoxycarbonyl)-L-tertiary leucine]amino}-4(S)-hydroxy-6-phenyl-2-azahexane VIII shown in the formula IX, wherein the compound shown in the formula IX is atazanavir. The method utilizes raw materials having a wide raw material source, the product is easy to purify, a cost is low, the synthesis processes are simple, the operation is simple, the process is simple, special requirement on equipment is avoided and large-scale production feasibility is realized.
Method for preparing anti-AIDS drug-Atazanavir monomer
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Paragraph 0022; 0023; 0024; 0025, (2017/06/02)
The invention discloses a method which is used for preparing an Atazanavir monomer and applied in the technical field of drug synthesis. The method comprises the steps that N-methoxycarbonyl-L-tertiary leucine and 1-[4-(pyridine-2-yl)-phenyl]-4(S)-hydroxyl-5(S)-2,5-diamido-6-phenyl-2-aza-hexane are subjected to an amidation reaction by taking HATU as a condensing agent under the condition of organic alkali and an organic solvent, certain aftertreatment is conducted, and then the Atazanavir monomer is obtained. According to the method, the synthetic yield of Atazanavir is increased, the purity is high, and the cost of raw materials is effectively reduced; meanwhile, the reaction time is short, material putting is easy, nitrogen protection is not needed, the material putting temperature can be properly controlled, by-products of HATU can be washed off more easily, the preparation time is greatly shortened, the working efficiency is improved, and therefore the method is suitable for industrial production.