- Preparation method ofdrug Rucaparib for treating ovarian cancer
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The invention discloses a preparation method of drug Rucaparib for treating an ovarian cancer. The method comprises the following steps that step 1, a compound A and a compound B with a PG protectinggroup are acylated in an organic solvent a under the action of an acid binding agent, and a compound of a formula I is prepared; step 2, an enamine bond of the compound of the formula I is hydrolyzedin an aqueous organic solvent b under the action of acid c to obtain a compound of a formula II; step 3, after the reduction of a nitro group to an amino group of the compound of formula II under theaction of a reducing agent, cyclodehydration is conducted to obtain a compound of a formula III; step 4, the compound of the formula III and N-(2-acetaldehyde) phthalimide are condensed under the action of acid d to obtain a compound of a formula IV; step 5, the compound of the formula IV is cyclized to obtain a compound of a formula V while removing the phthaloyl protecting group; step 6, the PGprotecting group of the compound of the formula V is removed to obtain the Rucaparib. The method reduces the cost of producing the drug Rucaparib for treating the ovarian cancer.
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Paragraph 0040
(2019/07/04)
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- METHODS AND INTERMEDIATES FOR PREPARING RUCAPARIB
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The present invention relates to a process for preparing rucaparib or pharmaceutically acceptable salts thereof. It also provides novel intermediates that may be converted into rucaparib or pharmaceutically acceptable salts thereof.
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- Method of preparing poly(ADP-ribose) polymerases inhibitors
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This invention relates to a new and convergent route to small molecule inhibitors of poly(ADP-ribose) polymerase, such as 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, via a key Sonogashira coupling reaction and a CuI-promoted indole formation.
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Page/Page column 6
(2010/10/20)
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