259796-12-8Relevant academic research and scientific papers
Preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline
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Paragraph 0019-0020; 0026-0029; 0039-0041, (2021/02/06)
The invention provides a preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline. The preparation method comprises the following steps: preparing a compound A by taking 3, 5-dichlorobenzoic acid as a raw material; preparing a compound B from the compound A; preparing a compound C from the compound B; preparing a compound D from the compound C; and obtaining a white solid 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline from the compound D. The preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline provided by the invention has the advantages of high product purity and high product yield.
N-(Substituted sulfonyl)benzamide derivative and preparation method and pharmaceutical application thereof
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Paragraph 0439; 0441; 0445-0448, (2019/04/17)
The invention relates to an N-(substituted sulfonyl)benzamide derivative and preparation method and pharmaceutical application thereof, in particular to an N-(substituted sulfonyl)benzamide derivativeshown as general formula (I), preparation method thereof, medicinal salts of the derivative, and their application as therapeutics, especially as Nav1.7 inhibitors, wherein substituents in the general formula (I) shown in the description are defined the same as in the description.
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors
Kishore Kumar,Chavarria, Gustavo E.,Charlton-Sevcik, Amanda K.,Arispe, Wara M.,MacDonough, Matthew T.,Strecker, Tracy E.,Chen, Shen-En,Siim, Bronwyn G.,Chaplin, David J.,Trawick, Mary Lynn,Pinney, Kevin G.
supporting information; experimental part, p. 1415 - 1419 (2010/07/06)
A small library of 36 functionalized benzophenone thiosemicarbazone analogs has been prepared by chemical synthesis and evaluated for their ability to inhibit the cysteine proteases cathepsin L and cathepsin B. Inhibitors of cathepsins L and B have the potential to limit or arrest cancer metastasis. The six most active inhibitors of cathepsin L (IC50 50 > 10,000 nM). The most active analog in the series, 3-bromophenyl-2′-fluorophenyl thiosemicarbazone 1, also efficiently inhibits cell invasion of the DU-145 human prostate cancer cell line.
Quinazoline derivatives useful in cancer treatment
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Page/Page column 208, (2010/11/25)
The present invention provides compounds of Formula I (wherein R1, R2, R3, L, and X are as defined herein). [image] or a pharmaceutically acceptable salt, solvate or ester thereof. The present invention also provides compositions comprising these compound
SUBSTITUTED PYRAZOLES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE
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Page/Page column 32, (2008/06/13)
The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes
A ROMPGEL-supported N-hydroxysuccinimide: A host of acylations with minimal purification
Barrett, Anthony G. M.,Cramp, Susan M.,Roberts, Richard S.,Zecri, Frederic J.
, p. 261 - 264 (2007/10/03)
(formula presented) amides, carbamates, ureas, Weinreb amides, hydroxamic acids Yields 89-98% Purity > 95% A novel N-hydroxysuccinimide ring-opening metathesis polymer is described as a recyclable supported acyl transfer reagent. Amides, carbamates, ureas, Weinreb amides, and hydroxamic acids are all obtained in excellent yields and purities from amines with minimal purification.
