253120-49-9Relevant academic research and scientific papers
A novel synthetic method for preparing an anticancer medicine Niraparib
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Page/Page column 8, (2017/08/02)
A novel synthetic method for preparing an anticancer medicine Niraparib is disclosed. The method includes subjecting an initial raw material that is 3-formyl-2-nitrobenzoic acid to 2-site nitro reduction, diazotization, reduction, cyclization, substitution, isomer resolution, amidation, and BOC removing to obtain the optically pure Niraparib the purity of which is 97.51% or above. The method is simple, convenient, high in yield, low in loss, easy to operate, low in equipment requirement and suitable for industrial production.
FIBROSIS INHIBITOR
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, (2008/06/13)
Medicament being useful as a fibrosis inhibitor for organs or tissues, which comprises a compound of the formula (I): wherein Ring Z is optionally substituted pyrrole ring, etc.; W2 is -CO-, -SO2-, optionally substituted C1-C4 alkylene, etc.; Ar2 is optionally substituted aryl, etc.; W1 and Ar1 mean the following (1) and (2):(1) W1 is optionally substituted C1-C4 alkylene, etc.; Ar1 is optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms:(2) W1 is optionally substituted C2-C5 alkylene, optionally substituted C2-C5 alkenylene, etc.; and Ar1 is aryl or monocyclic heteroaryl, which is substituted by carboxyl, alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof.
Pyrrole derivatives
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, (2008/06/13)
Pyrrole derivatives represented by the following formula: wherein Ring Z is an optionally substituted pyrrole ring, etc.; W2 is —CO—, —SO2—, an optionally substituted C1-C4 alkylene, etc.; Ar2 is an optionally substituted aryl, etc.; W2 and Ar1 mean the following (1) and (2): (1) W1 is an optionally substituted C1-C4 alkylene, etc.; Ar1 is an optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms: (2) W1 is an optionally substituted C2-C5 alkylene, an optionally substituted C2-C5 alkenylene, etc.; and Ar1 is an aryl or monocyclic heteroaryl, which are substituted by carboxyl, an alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof These compounds are useful as medicaments such as a fibrosis inhibitor for organs or tissues.
A preparation of methyl 2-amino-3-formylbenzoate and its use in Friedlander synthesis
Bu, Xianyong,Deady, Leslie W.
, p. 4223 - 4233 (2007/10/03)
The title compound has been prepared in four steps from methyl isatin-7- carboxylate. Condensations with 1-indanone and analogs gave 11H-indeno[1,2- b]quinoline-6-carboxylic acids, and with cyclohexanones gave acridine-4- carboxylic acids.
