22706-01-0

Upstream product

• 501-53-1 benzyl chloroformate 
• 95-54-5 1,2-diamino-benzene 
• 88-74-4 2-nitro-aniline 
• 23091-35-2 (2-nitrophenyl)carbamic acid benzyl ester 
• 13139-17-8 N-(Benzyloxycarbonyloxy)succinimide 

Downstream Products

• 57710-80-2 1-benzyloxycarbonyl-1Hbenzo[d][1.2.3]triazole 
• 95-54-5 1,2-diamino-benzene 
• 1312616-03-7 acetic acid 2-methyl-5-(methyl-pyridin-2-ylmethyl-amino)-4-[2-(methyl-pyridin-2-ylmethyl-amino)-phenylazo]-phenyl ester 
• 1312615-99-8 acetic acid 2-methyl-5-(methyl-pyridin-2-ylmethyl-amino)-4-[2-(methyl-pyridin-2-ylmethyl-amino)-phenylazo]-phenyl ester 
• 1312615-98-7 2-methyl-5-(methyl-pyridin-2-ylmethyl-amino)-4-[2-(methyl-pyridin-2-ylmethyl-amino)-phenylazo]-phenyl methyl ether 
• 1312615-97-6 2-methyl-5-(methyl-pyridin-2-ylmethyl-amino)-4-[2-(methyl-pyridin-2-ylmethyl-amino)-phenylazo]-phenol 
• 1154878-10-0 C₁₃H₁₅N₃ 
• 1312616-02-6 [2-(methyl-pyridin-2-ylmethyl-amino)-phenyl]carbamic acid benzyl ester 
• 1312616-01-5 {2-[(pyridin-2-ylmethyl)-amino]-phenyl}carbamic acid benzyl ester 
• 745824-90-2 C₂₈H₃₆FN₃O₆ 

Relevant academic research and scientific papers

Synthesis of Structurally Diverse Benzotriazoles via Rapid Diazotization and Intramolecular Cyclization of 1,2-Aryldiamines

An operationally simple method has been developed for the preparation of N-unsubstituted benzotriazoles by diazotization and intramolecular cyclization of a wide range of 1,2-aryldiamines under mild conditions, using a polymer-supported nitrite reagent and p-tosic acid. The functional group tolerance of this approach was further demonstrated with effective activation and cyclization of N-alkyl, -aryl, and -acyl ortho-aminoanilines leading to the synthesis of N1-substituted benzotriazoles. The synthetic utility of this one-pot heterocyclization process was exemplified with the preparation of a number of biologically and medicinally important benzotriazole scaffolds, including an α-amino acid analogue.

A protic ionic liquid catalyzed strategy for selective hydrolytic cleavage of tert-butyloxycarbonyl amine (N-Boc)

A simple, mild and efficient strategy for selective hydrolytic cleavage of the N-tert-butyloxycarbonyl (Boc) group is devised using a protic ionic liquid as an efficient catalyst. The deprotection reaction proceeded well for N-Boc protected aromatic, heteroaromatic, aliphatic compounds, and chiral amino acid esters and peptides. A wide range of labile protecting groups such as tert-butyl ester, tert-butyl ether, benzyloxycarbonyl (Cbz), TBDMS, O-Boc and S-Boc remained unaffected under the reaction conditions. This journal is

Short-circuiting azobenzene photoisomerization with electron-donating substituents and reactivating the photochemistry with chemical modification

Azobenzene (AB undergoes (E → (Z isomerization upon exposure to light. Whereas the light-induced structural change can be exploited for numerous applications, a second, light-orthogonal switch would facilitate the development of new uses for AB derivative

Bisphosphonate inhibition of the exopolyphosphatase activity of the Trypanosoma brucei soluble vacuolar pyrophosphatase

Trypanosoma brucei, the causative agent of African trypanosomiasis, contains a soluble, vacuolar pyrophosphatase, TbVSP1, not present in humans, which is essential for the growth of bloodstream forms in their mammalian host. Here, we report the inhibition of a recombinant TbVSP1 expressed in Escherichia coli by a panel of 81 bisphosphonates. The IC50 values were found to vary from ～2 to 850 μM. We then used 3D QSAR (comparative molecular field and comparative molecular similarity index; CoMFA and CoMSIA) methods to analyze the enzyme inhibition results. The R2 values for the experimental versus the QSAR-predicted activities were 0.78 or 0.61 for CoMFA and 0.79 or 0.68 for CoMSIA, for two different alignments. The root-mean-square (rms) pIC50 error for the best CoMFA model was 0.41 for five test sets of five activity predictions, which translates to a factor of ～2.6 error in IC50 prediction. For CoMSIA, the rms pIC50 error and error factors were 0.35 and 2.2, respectively. In general, the most active compounds contained both a single aromatic ring and a hydrogen bond donor feature. Thirteen of the more potent compounds were then tested in vivo in a mouse model of T. brucei infection. The most active compound in vivo provided a 40% protection from death with no apparent side effects, suggesting that further development of such compounds may be of interest.

ZN -CHELATING MOTIF-TETHERED SHORT -CHAIN FATTY ACIDS AS A NOVEL CLASS OF HISTONE DEACETYLASE INHIBITORS

Zn -chelating motif-tethered fatty acids as histone deacetylase (HDAC) inhibitors. Compounds performed well in in vitro and in vivo tests.

INDOLES, BENZIMIDAZOLES OR NAPHHIMIDAZOLES AS HISZONE DEACETYLASE (HDAC) INHIBITOR

A compound of the following formula (I):whereinR?1? is acyl, R?2? is hydrogen, orR?1? and R?2? are linked together to form a heterocyclic ring, R?5? is hydroxy, hydroxylamino, lower alkyl, lower alkoxy, halo(lower)alkyl or hydroxy(lower)alkyl, Q is lower