- Asymmetric synthesis of tetrahydropyran[3,2-c]quinolinones via an organocatalyzed formal [3 + 3] annulation of quinolinones and MBH 2-naphthoates of nitroolefin
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An efficient asymmetric and enantio-swithchable organocatalytic [3 + 3] annulation reaction using MBH-2-naphthoates of nitroalkenes and 4-hydroxyquinolin-2(1H)-ones has been developed. Densely substituted tetrahydropyrano[3,2-c]quinolinones scaffolds with two adjacent stereogenic centers are obtained with high yield (up to 95% yield) and good stereoselectivities (up to >20:1 dr and 96% ee) in an enantio-switchable manner. Furthermore, gram scale synthesis was achieved and the nitro group could easily transform into an amino group without any appreciable loss in the diastereo- and enantioselectivity.
- Li, Jian,Hu, Qi-Long,Chen, Xue-Ping,Hou, Ke-Qiang,Chan, Albert S.C.,Xiong, Xiao-Feng
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p. 697 - 700
(2019/09/30)
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- Alkyl and acyl substituted quinolines
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Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: STR1 and their pharmaceutically acceptable salts and solvates; wherein: (A) X is selected from
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- Acyl and alkoxy substituted quinolines
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Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are are represented by compounds of Formula 1.0: STR1 and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 and methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed. Also disclosed are compounds useful as antihypertensive agents and methods of treating hypertension using such compounds. The antihypertensive agents are compounds represented by Formula 1.0 wherein R4 is selected from the group consisting of alkyl and aminoalkyl. Preferably R1 is H.
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- Ester and alkoxy substituted benzopyrans
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Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: STR1 and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension using compounds of Formula 1.0 wherein R is selected from the group consisting of H, halogen and --C(O)OR6 ; and R1 is selected from the group consisting of --OR14, --O(CH2)a C(H)3-i Zi and --O(CH2)h N(R15)2.
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- Quinoline-diones
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Compounds of the formula STR1 or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C1 -C6) alkyl, N(C1 -C6 alkyl/aryl)2, OH, O--(C1 -C6) alkyl/aryl, CH2 OH, COOH, COO-alkyl/aryl, SO2 NH2, or SO2 NH (C1 -C6 alkyl/aryl); R1 is C1 -C6 alkyl, cycloalkyl, C2 -C6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH2 -aryl, --CH2 -substituted aryl, --CH2 -heteroaryl, or --CH2 -substituted heteroaryl; R2 is H, C1 -C6 alkyl or aryl; STR2 is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl) are described. These compounds are useful as agents for treating viruses.
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- Antiviral compounds and antihypertensive compounds
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Compounds useful as antihypertensive agents, or antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: STR1 and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension or a viral infection using compounds represented by Formulas 1.0. Also disclosed is a compound of Structure B STR2 useful as an intermediate in producing compounds of Formula 1.0. A process for preparing the compounds of Formula 1.0 is also disclosed. In the process a compound of Structure B STR3 is reacted with an alkoxide R1 O- M+ in a solvent comprising the corresponding alcohol R1 OH of the alkoxide. Optionally, an organic cosolvent may be used with the solvent.
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