182499-80-5

Upstream product

• 15864-32-1 2-amino-6-bromobenzothiazole 
• 62266-82-4 6-bromo-1,3-benzothiazol-2(3H)-one 
• 1306756-67-1 N,N'-(2,2'-disulfanediylbis(4-bromo-2,1-phenylene))diformamide 
• 106-40-1 4-bromo-aniline 
• 23451-95-8 2-amino-5-bromobenzenethiol 
• 321-23-3 4-bromo-2-fluoronitrobenzene 

Downstream Products

• 23451-95-8 2-amino-5-bromobenzenethiol 
• 875895-87-7 [2-(2-amino-5-bromo-phenylsulfanylmethyl)-phenyl]-methanol 
• 875895-75-3 2-(2-amino-5-bromo-phenylsulfanylmethyl)-benzoic acid methyl ester 
• 791614-78-3 ethyl 2-(6-bromobenzo[d]thiazol-2-yl)acetate 
• 791614-79-4 7-bromo-3-hydroxy-4H-benzo[1,4]thiazine-2-carboxylic acid ethyl ester 
• 1235453-34-5 6-bromo-2-(2-chlorophenyl)benzo[d]thiazole 
• 1235453-31-2 6-bromo-2-(4-iodophenyl)benzo[d]thiazole 
• 566169-97-9 2-(4’-aminophenyl)-6-bromobenzothiazole 
• 10544-50-0 sulfur 
• 51618-30-5 6-bromo-2-mercaptobenzothiazole 

Relevant academic research and scientific papers

Development of a radioiodinated thioflavin-T-Congo-red hybrid probe for diagnosis of systemic amyloidosis

Introduction: Systemic amyloidosis is a group of diseases characterized by the deposition of amyloid protein in multiple organs throughout the body and causing their dysfunction. As amyloid deposition is observed at an early phase and is highly specific t

Tricyclic oxazolidone comound, and preparation method and use thereof

The invention relates to a novel tricyclic oxazolidone comound, and a preparation method and a use thereof, and concretely discloses a compound with the structure represented by formula I, an enantiomer, a diastereomer or a raceme thereof or a mixture of the enantiomer, the diastereomer and the raceme, or a pharmaceutically acceptable salt thereof. The formula I is shown in the specification. The invention also discloses a preparation method of the compound, and an application of the compound in FXa target related disease treatment drugs.

Scalable synthesis of a cis-substituted cyclobutyl-benzothiazole pyridazinone: Process development of an efficient copper catalyzed C-N cross-coupling reaction

A scalable process for the preparation of 2-(2-(cis-3-(piperidin-1-yl) cyclobutyl)benzothiazol-6-yl)pyridazin- 3(2H)-one in multi-kilogram amounts and in high purity has been developed. The key features of this synthesis are the coppercatalyzed C-N cross-

Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor

The blood coagulation enzyme factor Xa (FXa) is a particularly promising target for anticoagulant therapy, and identification of oral small-molecule inhibitors of FXa remains a research focus. On the basis of the X-ray crystal structure of FXa and its inhibitor rivaroxaban, we designed and synthesized a series of conformationally restricted mimics containing a novel [6,6,5] tricyclic fused oxazolidinone scaffold. Intensive structure-activity relationship (SAR) and structure-pharmacokinetic relationship (SPR) studies on this new series led to the discovery of compound 11a: a highly potent, selective, direct, and orally bioavailable FXa inhibitor with excellent in vivo antithrombotic efficacy and preferable pharmacokinetic profiles. Druggability evaluation of compound 11a was undertaken and elicited positive outcomes. All results indicate that compound 11a is a promising drug candidate for the prevention and treatment of thromboembolic diseases in venous and arterial systems.

Fluorescence properties of 5-(5,6-dimethoxybenzothiazol-2-yl)-2′- deoxyuridine (dbtU) and oligodeoxyribonucleotides containing d btU

We describe the synthesis and photophysical properties of 11 substituted 5-(benzothiazol-2-yl)-2′-deoxyuridine derivatives and oligodeoxyribonucleotides (ODNs) containing 5-(5,6-dimethoxybenzothiazol-2-yl)- 2′-deoxyuridine (dbtU), which was the strongest fluorescent derivative among those prepared. The fluorescence properties of dbtU itself and ODNs containing dbtU show the same tendency of being weaker in both neutral and acidic solution and stronger in basic solution. The ODNs (15mer) containing 16 combinations of 5′-XbtU-3′ and 5′-btUY-3′, where X, Y = A, T, G, or C, were synthesized, and their fluorescence intensity and quantum yield in basic solution were compared. On average, only the ODN with the 5′-G btU-3′ sequence shows a 7.9-fold lower fluorescence intensity than the other sequences. Ab initio calculations of 5′-G btU-3′ and 5′-btUG-3′ as models under basic conditions suggest that the lower fluorescence of the ODN containing the 5′-GbtU-3′ sequence is caused by a wider overlap between stacked guanine (Gua) and btUra than that of the 5′- btUG-3′ sequence and that the HOMO is delocalized not only on btUra but also on Gua.

Copper-catalyzed activation of disulfides as a key step in the synthesis of benzothiazole moieties

A convenient synthesis of substituted benzothiazoles has been accomplished by way of a copper catalyzed reaction of aromatic disulfide amines and aldehydes. The process, which involves copper catalyzed activation of disulfide functionality, proceeds in a

Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5- fluorobenzothiazole (PMX 610, NSC 721648)

New fluorinated 2-aryl-benzothiazoles, -benzoxazoles, and -chromen-4-ones have been synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole 5. Analogues such as 9a,b and 12a,d yielded submicromolar GI50 values in both cell lines; however, none of the new compounds approached 5 in terms of antitumor potency. For 5, binding to the aryl hydrocarbon receptor appeared to be necessary but not sufficient for growth inhibition.

Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17β-hydroxysteroid dehydrogenase type 3

A novel series of 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitors has been identified. These inhibitors, based on a dibenzazocine core, exhibited picomolar to low nanomolar inhibition of 17β-HSD3 in cell-free enzymatic as well as in cell-based transcriptional reporter assays.

Fused bicyclic-substituted amines as histamine-3 receptor ligands

Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.

Fused bicyclic-substituted amines as histamine-3 receptor ligands

Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.