115913-31-0Relevant articles and documents
Bridge-Chlorinated Bicyclo[1.1.1]pentane-1,3-dicarboxylic Acids
Kaleta, Ji?í,Ron?evi?, Igor,Císa?ová, Ivana,Dra?ínsky, Martin,?olínová, Veronika,Ka?i?ka, Václav,Michl, Josef
, p. 2448 - 2461 (2019)
Radical chlorination of bicyclo[1.1.1]pentane-1,3-dicarboxylic acid is highly selective, and up to four chlorine atoms can be introduced relatively easily without damage to the strained bicyclic cage. Combined with hydrodechlorination with TMS3SiH, direct chlorination provides access to five of the 15 possible chlorinated diacids. Their configuration has been established by X-ray diffraction. Their pKa values have been measured by capillary electrophoresis and calculated at the B3LYP-D3BJ/6-311+G(d,p)-level. The results are in good agreement and reflect the expected trend, from 2.78 ± 0.08 and 4.14 ± 0.10 in the parent to 1.07 ± 0.03 and 2.31 ± 0.03 in the tetrachlorinated diacid. Strain energy relative to the parent diacid was calculated for all 15 chlorinated diacids and shows a dramatic increase with successive chlorination, due to nonbonded Cl-Cl repulsions.
DEOXYNOJIRIMYCIN DERIVATIVES AS GLUCOSIDASE INHIBITORS
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Paragraph 0655, (2022/01/22)
The present invention relates to novel iminosugars and their use as glucosidase inhibitors. The present inventors discovered that certain deoxynojirimycin derivatives may be effective in inhibiting glucosidases. In particular, such deoxynojirimycin derivatives may be useful for treating a disease or condition in which inhibition of glucosidase may play an important role.
Preparation method for bicyclo [1.1.1] pentane-1,3-dicarboxylic acid dimethylester
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Paragraph 0006; 0013, (2017/03/08)
The invention relates to a preparation method for bicyclo [1.1.1] pentane-1,3-dicarboxylic acid dimethylester, and mainly solves the technical problem that a method suitable for industrial synthesis does not exist at present. The preparation method comprises the following six steps: firstly, reacting a compound (1) and bromoform under an alkaline condition to obtain a compound (2); secondly, reacting the compound (2) and lithium methide to obtain a compound (3); thirdly, illuminating the compound (3) and diacetyl by a high-pressure mercury lamp to obtain a compound (4); fourthly, treating with sodium hypochlorite to obtain a compound (5); fifthly, reacting the compound (5) and thionyl chloride to obtain a compound (6); and finally, treating the compound (6) under the effect of methanol to obtain a compound (7) which is a final product. A reaction formula is as shown in the specification, and the acquired bicyclo [1.1.1] pentane-1,3-dicarboxylic acid dimethylester is a useful midbody or product for synthesis of many drugs.