- Preparation method of veliparib
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The invention discloses a preparation method of veliparib, which comprises the following steps: by using readily available L-alanine ethyl ester as a raw material, carrying out imidization, cyclization reduction and hydrolysis reaction to obtain a key chiral intermediate that is (R)-2-methylpyrrolidine-2-carboxylic acid, and carrying out one-step condensation on the intermediate to obtain the target compound veliparib. The method has the characteristics of easily available raw materials, mild conditions, simple process, safety, environmental protection and the like, and is suitable for industrial production.
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- Synthesis of (R)-Boc-2-methylproline via a Memory of Chirality Cyclization. Application to the Synthesis of Veliparib, a Poly(ADP-ribose) Polymerase Inhibitor
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(R)-Boc-2-methylproline (3a) was synthesized in good yield with excellent stereochemical control from alanine benzyl ester hydrochloride 11. The process, which is based on a modification of one described by Kawabata, proceeds in four steps and requires no
- Kolaczkowski, Lawrence,Barkalow, Jufang,Barnes, David M.,Haight, Anthony,Pritts, Wayne,Schellinger, Adam
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p. 4837 - 4845
(2019/03/07)
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- Method for preparing (R)-2-(2-methylpyrrolidine-2-yl)-1H-benzimidazole-4-carboxamide
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The invention relates to a method for preparing (R)-2-(2-methylpyrrolidine-2-yl)-1H-benzimidazole-4-carboxamide. The method has the advantages of avoiding of trifluoroacetic acid and other strong acids, simplification of present preparation technologies, pollution reduction, cost reduction, and improvement of the purity and the yield of the above product.
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Paragraph 0040-0050
(2017/03/17)
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- 2-{(R)-2-METHYLPYRROLIDIN-2-YL)-1H-BENZIMIDAZOLE-4-CARBOXAMIDE CRYSTALLINE FORM 1
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2-((R)-2-Methylpyrrolidin-2-yl)-1H-benzimidazole-4-carboxamide Crystalline Form 1, ways to make it, compositions comprising it and made using it, and methods of treating patients having disease using it are disclosed.
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Page/Page column 6
(2009/04/24)
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- 2-{(R)-2-METHYLPYRROLIDIN-2-YL)-1H-BENZIMIDAZOLE-4-CARBOXAMIDE CRYSTALLINE FORM 2
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2-((R)-2-Methylpyrrolidin-2-yl)- I H-benzimidazole-4-carboxamide Crystalline Form 2, ways to make it, compositions comprising it and made using it, and methods of treating patients having disease using it are disclosed.
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Page/Page column 5-6
(2009/04/24)
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