1335210-24-6Relevant articles and documents
Cabotegravir derivative with biological activity as well as preparation method and application thereof
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Paragraph 0068-0070, (2021/10/27)
The invention belongs to the technical field of chemical synthesis of medicines, and particularly relates to a cabotegravir derivative with biological activity as well as a preparation method and application thereof. The structural formula of the cabotegravir derivative is shown in the specification, wherein R1 is methyl or hydrogen; R2 is methylene, 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, nitrogen-containing heterocyclic ring, sulfur-containing heterocyclic ring or oxygen-containing heterocyclic ring. The preparation method comprises the following steps of: carrying out deprotection on 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, and carrying out acylation reaction on the cyclized aldehyde and an amino compound; or firstly reacting the aldehyde with an amino compound, and then cyclizing with aminopropanol; 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.
An Efficient and Highly Diastereoselective Synthesis of GSK1265744, a Potent HIV Integrase Inhibitor
Wang, Huan,Kowalski, Matthew D.,Lakdawala, Ami S.,Vogt, Frederick G.,Wu, Lianming
supporting information, p. 564 - 567 (2015/03/04)
A novel synthesis of GSK1265744, a potent HIV integrase inhibitor, is described. The synthesis is highlighted by an efficient construction of the densely functionalized pyridinone core as well as a highly diastereoselective formation of the acyl oxazolidine moiety. The latter exploits the target molecules ability to chelate to Mg2+, a key feature in the integrase inhibitors mechanism of action.