- Cabotegravir derivative with biological activity as well as preparation method and application thereof
-
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.
- -
-
Paragraph 0068-0070
(2021/10/27)
-
- CONTINUES FLOW PROCESS FOR THE PREPARATION OF ACTIVE PHARMACEUTICAL INGREDIENTS - POLYCYCLIC CARBAMOYL PYRIDONE DERIVATIVES AND INTERMEDIATES THEREOF
-
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).
- -
-
-
- An Efficient and Highly Diastereoselective Synthesis of GSK1265744, a Potent HIV Integrase Inhibitor
-
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.
- Wang, Huan,Kowalski, Matthew D.,Lakdawala, Ami S.,Vogt, Frederick G.,Wu, Lianming
-
p. 564 - 567
(2015/03/04)
-
- PROCESS FOR PREPARING CARBAMOYLPYRIDONE DERIVATIVES AND INTERMEDIATES
-
The present invention relates to the preparation of carbamoylpyridone derivatives and intermediates.
- -
-
-