- Dolutegravir derivative with biological activity as well as preparation method and application thereof
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The invention relates to the technical field of pharmaceutical chemistry synthesis, in particular to a dolutegravir derivative with biological activity and a preparation method thereof. The structural formula of the derivative is shown in the specification, wherein R1 is methyl or hydrogen; R2 is methyl, isopropyl, phenyl, benzyl, a nitrogen-containing heterocyclic ring, a sulfur-containing heterocyclic ring or an oxygen-containing heterocyclic ring; and R3 is hydrogen, methyl, ethyl, phenyl, benzyl, a nitrogen-containing heterocyclic ring, a sulfur-containing heterocyclic ring or an oxygen-containing heterocyclic ring. The preparation method comprises the following steps of: deprotecting 1-(2, 2-dimethoxyethyl)-1, 4-dihydro-3-methoxy-4-oxo-2, 5-pyridinedicarboxylic acid-2-methyl ester to obtain aldehyde, cyclizing the aldehyde with aminobutanol, then carrying out acylation reaction on the cyclized aldehyde and an amino compound, and finally carrying out click reaction with azide to obtain a target compound. The derivative provided by the invention has proliferation inhibition activity on human tumor cells.
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Paragraph 0067-0075
(2021/10/27)
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- Triazole derivative with tumor cell calcium ion channel and preparation method and application thereof
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The invention relates to the technical field of pharmaceutical chemistry synthesis, in particular to a triazole derivative with a tumor cell calcium ion channel and a preparation method and application thereof. By click reaction, benzyl in the structure is changed to 1, 2 and 3 - triazole structures to obtain a novel compound, can inhibit growth of tumor cells by influencing calcium ion channels in tumor cells, and has remarkable application value.
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Paragraph 0141-0143
(2021/10/27)
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- CONTINUES FLOW PROCESS FOR THE PREPARATION OF ACTIVE PHARMACEUTICAL INGREDIENTS - POLYCYCLIC CARBAMOYL PYRIDONE DERIVATIVES AND INTERMEDIATES THEREOF
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The present invention discloses continues flow process for the preparation of polycyclic carbamoyl pyridone derivatives and intermediates thereof. In particular, the present invention discloses a process for the preparation of intermediate. Formule (V).
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- A kind of improved lu tewei preparation process (by machine translation)
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The present invention provides anti-aids drugs lu tewei improved preparation process, and for lu tewei bulk drug process control study of the diastereoisomeric synthetic intermediates 6' and its preparation method. The process for preparing the simple routes, simplified for intermediate purification processing, in addition this invention obtained the diastereoisomeric synthetic intermediates 6' help for lu tewei raw material preparation process of quality research. (by machine translation)
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- Preparation of Dolutegravir Intermediate Diastereomer
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A convenient method was developed to prepare the diastereomer of dolutegravir tricyclic intermediate in the catalysis of EDCI/DMAP in up to 87% yield. Different solvents, temperature, and times were optimized. The synthesized diastereomer 6′ could be used as a standard for the industrial manufacture requirement of dolutegravir active pharmaceutical ingredient.
- Wang, Xianheng,Chen, Song,Zhao, Changkuo,Long, Liangye,Wang, Yuhe
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- PROCESS FOR THE PREPARATION OF DOLUTE-GRAVIR AND INTERMEDIATES THEREOF
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The present disclosure relates to processes for the preparation of dolutegravir or of its pharmaceutically acceptable salts. The present disclosure also provides intermediates useful in the synthesis of dolutegravir.
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- AN IMPROVED PROCESS FOR THE PREPARATION OF DOLUTEGRAVIR
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The present invention provides (R)-3-Amino-1-butanol (D)-tartarate (lIb); process for its preparation and its conversion to Dolutegravir. The present invention also provides an improved process for the preparation of Dolutegravir (I) or pharmaceutically acceptable salts wherein compound (XVI) is reacted with an optically active acid addition salt of (R)-3-amino-1-butanol (lla).
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Page/Page column 21
(2014/09/03)
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