- Synthesis method of 2-methyl-1, 2, 4-triazole-3-amine
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The invention relates to a synthesis method of 2-methyl-1, 2, 4-triazole-3-amine, and mainly solves the technical problem that no suitable industrial synthesis method exists at present. The method comprises the following three steps: 1, reacting a compound 1 in a solvent 1, 4-dioxane with added N, N-dimethylformamide dimethyl acetal to obtain a compound 2; 2, reacting the compound 2 with triphenylphosphine and diisopropyl azodicarboxylate in methanol to obtain a compound 3; and 3, reacting the compound 3 with sodium hydroxide in methanol and water to obtain a final compound 4, wherein the reaction formula is described in the specification.
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Paragraph 0007; 0009
(2020/09/16)
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- Structure-activity relationships of triazole-benzodioxine inhibitors of cathepsin X
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Cathepsin X is a cysteine carboxypeptidase that is involved in various physiological and pathological processes. In particular, highly elevated expression and activity of cathepsin X has been observed in cancers and neurodegenerative diseases. Previously, we identified compound Z9 (1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2-((4-isopropyl-4H-1,2,4-triazol-3-yl)thio)ethan-1-one) as a potent and specific reversible cathepsin X inhibitor. Here, we have explored the effects of chemical variations to Z9 of either benzodioxine or triazol moieties, and the importance of the central ketomethylenethio linker. The ketomethylenethio linker was crucial for cathepsin X inhibition, whereas changes of the triazole heterocycle did not alter the inhibitory potencies to a greater extent. Replacement of benzodioxine moiety with substituted benzenes reduced cathepsin X inhibition. Overall, several synthesized compounds showed similar or improved inhibitory potencies against cathepsin X compared to Z9, with IC50 values of 7.1 μM–13.6 μM. Additionally, 25 inhibited prostate cancer cell migration by 21%, which is under the control of cathepsin X.
- Fonovi?, Ur?a Pe?ar,Gobec, Stanislav,Hrast, Martina,Knez, Damijan,Kos, Janko,Proj, Matic,Zidar, Nace
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- Synthesis of 1-Alkyl-5-amino-1,2,4-triazoles Based on Nucleophilic Substitution and Reduction Reactions
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A series of 1-alkyl-5-amino-1H-1,2,4-triazoles were synthesized starting from 3,5-dibromo-1H- 1,2,4-triazole by alkylation and subsequent nucleophilic substitution of the 5-bromine atom by azido group, reduction of the latter to amino group, and hydrodebromination.
- Tolstyakov
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p. 1537 - 1547
(2019/01/04)
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- Deacetylcolchicine deriv.
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Provided are 4-modified colchicine compounds and medicines using the same. Specifically provided are colchicine derivatives represented by general formula (1), salts thereof, and solvates of the same. In general formula (1), R1 is a halogen atom, a hydroxyl group, a nitro group, an amino group, or a mono-, di- or tri-fluoromethyl group; R2, R3 and R4 are each a methoxy group or a hydroxyl group, or alternatively R2 and R3, or R3 and R4 together represent a methylenedioxy group; R5 and R6 may be the same or different and are each a hydrogen atom, a C1-6 alkyl group, an arylalkyl group, a C2-6 alkenyl group, -COR7, -COOR8, -SO2R9, -CONR10R11, or -CSNR12R13, or alternatively R5 and R6 together with the nitrogen atom to which R5 and R6 are bonded may form a three- to seven-membered cyclic amino group; R7 is a C1-6 alkyl group or the like; R8 is a C1-6 alkyl group or the like; R9 is a C1-6 alkyl group or the like; R10 and R11 may be the same or different and are each a hydrogen atom, a C1-6 alkyl group, or the like; and R12 and R13 may be the same or different and are each a hydrogen atom, an alkyl group, or the like.
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Paragraph 0501
(2016/10/08)
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- Development of a scaleable process for the synthesis of a next-generation statin
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This manuscript details the process research and development of a convergent and safe approach to 1 on a multikilo scale. Specific highlights of the process development efforts will be described, including the development of a dehydrogenation method for d
- Hobson, Lindsay A.,Akiti, Otute,Deshmukh, Subodh S.,Harper, Shannon,Katipally, Kishta,Lai, Chiajen J.,Livingston, Robert C.,Lo, Ehrlic,Miller, Michael M.,Ramakrishnan, Srividya,Shen, Lifen,Spink, Jan,Tummala, Srinivas,Wei, Chenkou,Yamamoto, Kana,Young, John,Parsons Jr., Rodney L.
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scheme or table
p. 441 - 458
(2011/04/22)
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