13037-63-3

Upstream product

• 463-71-8 thiophosgene 
• 615-57-6 2,4-dibromo-aniline 
• 454426-44-9 N-(2,4-dibromo-phenyl)-N'-phenyl-thiourea 
• 594-42-3 chlorothio-trichloro-methane 
• 1985-12-2 4-Bromophenyl isothiocyanate 
• 75-15-0 carbon disulfide 
• 1189351-07-2 C₆H₁₅N*C₇H₅Br₂NS₂ 
• 23373-04-8 2',4'-dibromoacetanilide 

Downstream Products

• 1161730-15-9 N-(2,4-dibromophenyl)-3-hydroxyazetidine-1-carbothioamide 
• 1189350-92-2 6-bromo-2-(phenylthio)-1,3-benzothiazole 
• 1199943-81-1 6-bromo-2-phenoxy-1,3-benzothiazole 
• 1580491-04-8 C₁₀H₁₂Br₂N₂OS 
• 863001-17-6 4-(6-bromobenzo[d]thiazol-2-yl)morpholine 
• 16691-32-0 1-(2,4-Dibrom-phenyl)-4-S-methyl-4-isodithiobiuret 
• 90617-75-7 (2,4-dibromo-phenyl)-thiourea 

Relevant academic research and scientific papers

Isothiocyanate-Directed Ortho-Selective Halogenation of Arenes via C–H Functionalization

Abstract: Ortho-selective halogenation of arenes via C–H functionalization has been described under mild reaction conditions. In this reaction Cu(II)X2 was used as a halide source. It is a simple, general and efficient method for the synthesis of 2-halo aromatic isothiocyanates. All the reactions are carried out under optimized reaction conditions to provide their respective desired products in good to high yield. Graphical Abstract: We have developed a general, simple and efficient method for the synthesis of 2-halo arylisothiocyanates from isothiocyanates through ortho-selective halogenation under mild reaction conditions. Cu(II)X2 was used as a halide source for this methodology. All the reactions are carried out under optimized reaction conditions to provide their respective desired products in good to high yield. [Figure not available: see fulltext.].

Synthesis and biological evaluation of terminal functionalized thiourea-containing dipeptides as antitumor agents

A series of antitumor agents based on terminal functionalized dipeptide derivatives containing the thiourea moiety were synthesized and evaluated for antiproliferative activity using a panel of cancer cell lines, and the effects and mechanism of apoptosis induction were determined. These compounds exhibited significant selectivity to different cancer cell lines with IC50 values at micromolar concentrations. In particular, compound I-11 appeared to be the most potent compound, with an IC50 = 4.85 ± 1.44 μM against the NCI-H460 cell line, at least partly, by the induction of apoptosis. Mechanistically, compound I-11 induced the activation of caspase-12 and CHOP, which triggered apoptotic signalling via the ROS-dependent endoplasmic reticulum pathway and arrested the cell cycle at the S phase. Thus, we concluded that dipeptide derivatives containing the thiourea moiety terminally functionalized by electron-withdrawing substituents may be potential antitumor agents for further investigation.

Convenient synthesis of benzo[4,5]thiazolo[2,3-c][1,2,4]triazoles with 1 mol% CuCl2·2H2O as catalyst in water

A convenient and efficient procedure for the synthesis of benzo[4,5]thiazolo [2,3-c][1,2,4]triazoles has been developed via a tandem intermolecular C-N bond and intramolecular C-S bond formation sequence from o-bromo-arylisothiocyanates and aroylhydrazides. A series of benzo[4,5]thiazolo[2,3-c][1,2,4]triazoles were provided in excellent overall yields with 1 mol% CuCl2·2H2O/1 mol% 1,10-phenanthroline as the catalyst and water as the solvent. This journal is

Design, synthesis and in vitro evaluation of novel ursolic acid derivatives as potential anticancer agents

A series of novel ursolic acid (UA) derivatives modified at the C-3 and the C-28 positions were designed and synthesized in an attempt to develop potential antitumor agents. The in vitro cytotoxicity were evaluated against five cancer cell lines (MGC-803, HCT-116, T24, HepG2 and A549 cell lines) and a normal cell (HL-7702) by MTT assay. The screening results indicated that some of these target compounds displayed moderate to high levels of antiproliferative activities compared with ursolic acid and 5-fluorouracil (5-FU), and exhibited much lower cytotoxicity than 5-FU, indicating that the targeted compounds had selective and significant effect on the cell lines. The induction of apoptosis and affects on the cell cycle distribution of compound 6r were investigated by acridine orange/ethidium bromide staining, Hoechst 33258 staining, JC-1 mitochondrial membrane potential staining and flow cytometry, which revealed that the antitumor activity of 6r was possibly achieved through the induction of cell apoptosis by G1 cell-cycle arrest. Western blot and qRT-PCR (quantitative real-time PCR) experiments demonstrated that compound 6r may induce apoptosis through both of intrinsic and extrinsic apoptosis pathway.

Structure-activity relationship of dihydroimidazo-, dihydropyrimido, tetrahydrodiazepino-[2,1-b]-thiazoles, and -benzothiazoles as an acylation catalyst

Cyclic isothioureas 1, 2, 3, and 4 were synthesized through a four-step procedure from the corresponding ortho-bromoanilines 10 via Pd- or Cu-catalyzed cyclization-benzothiazole formation. Nonbenzo analogues 7, 8, and 9 were synthesized by a condensation reaction of cyclic thioureas 15 and α-bromoacetophenones 14. Investigations of the acylation reactions of 1-phenylethanol with acid anhydrides in the presence of these cyclic isothiourea catalysts revealed their structure-activity relationships. Remarkable electronic effects resulting from substituent(s) on a benzo or phenyl moiety and the influence of the size of the annulating ring were observed. Introduction of an electron-donating substituent(s) enhanced the reaction rate. A few substitution effects on chiral catalysts of type 3 and 7 were also studied.

TRI-CYCLIC PYRAZOLOPYRIDINE KINASE INHIBITORS

The present invention relates to compounds useful as inhibitors of P13K, particularly of P13Kgamma. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of several diseases, such as cancer and autoimmune diseases.

Copper(I)-catalyzed cascade synthesis of 2-substituted 1,3-benzothiazoles: Direct access to benzothiazolones

An efficient cascade process for the preparation of 2-substituted 1,3-benzothiazoles directly from 2-haloaryl isothiocyanates and O or S nucleophiles by a Cu-catalyzed, intramolecular, C-S bond formation has been developed. This cascade method is viable f

Alkanimidoylthioureas

The compounds of this invention are novel alkanimidoylthioureas having antifertility activity. They are prepared by the reaction of appropriate alkanamidines with appropriate isothiocyanates.