5442-12-6Relevant articles and documents
Norcantharidin carboxylic acid monofluorobenzyl ester and synthesis method and anti-tumor application thereof
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Paragraph 0028; 0036-0037, (2020/07/02)
The invention provides synthesis and anti-tumor application of norcantharidin carboxylic acid monofluorobenzyl ester with a structural formula shown as I in the specification. The specific structure of the norcantharidin carboxylic acid monofluorobenzyl ester as shown in the formula I is shown in the specification, and activity tests show that the norcantharidin carboxylic acid monofluorobenzyl ester as shown in the formula I, which is designed and synthesized by the invention, is a suitable anti-tumor candidate drug, especially as an anti-liver cancer candidate drug. Compared with a positivecontrol drug norcantharidin, the norcantharidin sodium salt has the advantage that the water solubility, the stability and the anti-tumor activity are improved. In addition, the synthesis method of norcantharidin carboxylic acid monofluorobenzyl ester has the advantages that the raw materials are easy to obtain, and the operation and the implementation are very easy.
Camptothecin-glycine-norcantharidin conjugate and application thereof
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Paragraph 0020; 0026; 0027, (2019/12/29)
The invention provides a camptothecin-glycine-norcantharidin conjugate I and a preparation method thereof. R in the formula I is selected from C1-C6 alkyl groups, substituted alkyl groups, cycloalkylgroups, benzyl groups or substituted benzyl groups. Activity tests prove that the designed and synthesized camptothecin-glycine-norcantharidin conjugate I has an excellent antitumor effect, and especially has high activity on liver cancer, stomach cancer, colon cancer and pancreatic cancer. Additionally, the preparation method of the camptothecin-glycine-norcantharidin conjugate I has the advantages of easily available raw materials, low cost, high yield of the target product, and easiness in preparation.
IMPROVED PROCESS FOR THE PREPARATION OF A BENZENE COMPOUND
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Page/Page column 12; 13, (2016/07/05)
A benzene compound is prepared in a process, which comprises (i) reacting a furan compound of formula (I): wherein R1 and R2 are the same or different and independently selected from the group consisting of hydrogen, alkyl, aralkyl, -CHO, -CH2OR3, -CH(OR4 )(OR5), -COOR6, wherein R3, R4 and R5 are the same or different and are independently selected from the group consisting of hydrogen, alkyl, aryl, alkaryl, aralkyl, alkylcarbonyl and arylcarbonyl, or wherein R4 and R5 together form an alkylene group, and wherein R6 is selected from the group consisting of hydrogen, alkyl and aryl, with an olefin of the formula (II): R7-CH=CH-R8; wherein R7 and R8 are the same or different and are independently selected from the group consisting of hydrogen, sulfonate, -CN, -CHO, and -COOR9, wherein R9 is selected from the group consisting of hydrogen, and an alkyl group, or R7 and R8 together form a –C(O)-O-(O)C- group or a –C(O)-NR10-C(O)- group, wherein R10 represents hydrogen, an aliphatic or an aromatic group, to produce an unsaturated bicyclic ether having an unsaturated carbon-carbon bond; (ii) hydrogenating the unsaturated carbon-carbon bond in the unsaturated bicyclic ether to produce a saturated bicyclic ether; and (iii) dehydrating and aromatizing the saturated bicyclic ether to produce the benzene compound.
