- Synthesis method of 4,7-diazaspiro[2.5]octane compound
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The invention discloses a synthesis method of a 4,7-diazaspiro[2.5]octane compound, which comprises the following steps: by using a derivative of 4-methoxybenzyl-(1-(hydroxymethyl) cyclopropyl) carbamate as a raw material, substituting, adding a protecting group, removing the protecting group, and performing reduction to obtain the 4,7-diazaspiro[2.5]octane compound. According to the method disclosed by the invention, a flammable and combustible boron trifluoride diethyl ether adduct with corrosive toxicity is prevented from being used in a synthesis route to carry out a synthesis reaction, and the safety in the synthesis reaction is improved.
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Paragraph 0081-0087
(2020/11/26)
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- Synthesis method of 4,7-diazaspiro[2.5]octane compound
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The invention discloses a synthesis method of a 4,7-diazaspiro[2.5]octane compound, which comprises the following steps: by using a derivative of 4-methoxybenzyl-(1-(hydroxymethyl)cyclopropyl) carbamate as a raw material, substituting, adding a protecting group, esterifying, re-substituting, and removing the protecting group to obtain the 4,7-diazaspiro[2.5]octane compound. According to the synthetic route, the 4,7-diazaspiro[2.5]octane compound (such as 7-benzyl-4,7-diazaspiro[2.5]octane in the scheme) is directly obtained through the last step of cyclization, so that the problem of carbon-oxygen double bond reduction in the existing literature is avoided.
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- Preparation method of 4,7-diazaspiro[2.5]octane derivative
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The invention provides a preparation method of 4,7-diazaspiro[2.5]octane derivative. The 4,7-diazaspiro[2.5]octane derivative is prepared by taking 1-aminocyclopropane carboxylate as a starting material. The preparation method has the advantages of simple operation steps, stable process conditions, high controllability, high product yield (the four-step reaction yield of compounds shown as formulas II to I can be up to 70 percent), environmental friendliness and the like, and is suitable for large-scale production.
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Paragraph 0073; 0083; 0084; 0085
(2018/12/13)
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- Sulfamide derivative and application thereof
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The invention relates to a sulfamide derivative and a pharmaceutical composition comprising the compound as well as use of the sulfamide derivative and the pharmaceutical composition as a preparation drug, in particular, use of a drug for preparing a BCL-2 family protein antagonist and use of the drug for treating cancers.
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Paragraph 0181; 0182
(2017/08/29)
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- IMIDAZOTHIAZOLE DERIVATIVE HAVING PROLINE RING STRUCTURE
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[Problem to be Solved] There is provided a novel compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. [Solution] The present invention provides an imidazothiazole derivative rep
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Page/Page column 55; 56
(2011/11/07)
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- MORPHOLINOPURINE DERIVATIVES
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There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: wherein R1, R2, R3, R4, Ra, Rb, Rc, and X each have the same meaning as defined in the specification.
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Page/Page column 154
(2010/06/14)
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