- A 3,4- [...] method for the synthesis of
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The invention discloses a novel synthesis method of 3,4-dichloropyridazine. The 3,4-dichloropyridazine 4 is prepared through reaction between a compound 3 and POCl3 in an isopropanol solvent, the compound 3 is prepared through reaction between a compound 2 and MnO2 in a tetrahydrofuran solvent, and the compound 2 is prepared through reaction between a compound 1 and hydrazine hydrate in an acetonitrile solvent, wherein preferred conditions are as follows: a mol ratio of the hydrazine hydrate to the compound 1 is 1.1 to 1, the reaction temperature is 25-30 DEG C, the time is 6h; a mol ratio of MnO2 to the compound 2 is 4 to 1, the reaction temperature is 25 DEG C, the time is 8h; a mol ratio of the POCl3 to the compound 2 is 2.5 to 1, the reflowing reaction temperature is 80 DEG C, and the time is 3h. The synthesis method has the advantages that the raw materials are easily available, reaction conditions are mild, operability in post-treatment is good, the yield is relatively high, the production is easily enlarged, and thus the novel synthesis method is especially suitable for industrial large-scale production.
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Paragraph 0034-0040
(2017/05/04)
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- HETEROCYCLIC ANTIVIRAL COMPOUNDS
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Compounds having the formula I wherein R1, R2, R3, R4, and R5 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV in
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Page/Page column 19-20
(2011/04/18)
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- HETEROCYCLIC ANTIVIRAL COMPOUNDS
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Compounds having the formula I wherein wherein R1, R2, R3b, R4a, R4b, R4c and as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods
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Page/Page column 26
(2010/12/29)
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- HETEROCYCLIC ANTIVIRAL COMPOUNDS
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Compounds having the formula I wherein R1, R2, R3, R4, R5a, R5b, R5c and R6 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are
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Page/Page column 42
(2010/11/05)
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- HETEROCYCLIC ANTIVIRAL COMPOUNDS
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Compounds having the formula I wherein wherein R1, R2, R3, R4, X1, X2, X3 and X4 and as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
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Page/Page column 41
(2010/12/29)
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- HETEROCYCLIC ANTIVIRAL COMPOUNDS
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Compounds having the formula I wherein A, R1, R2, R3, R4a, R4b, R4c, R5, R6, R7a, R7b, Ar1, Rc, Rd, Re/sup
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