87107-79-7

Upstream product

• 136918-14-4 phthalimide 
• 622-08-2 2-Benzyloxyethanol 
• 3891-07-4 N-(2-Hydroxyethyl)phthalimide 
• 100-39-0 benzyl bromide 
• 85-44-9 phthalic anhydride 

Downstream Products

• 38336-04-8 O-benzylethanolamine 
• 328031-28-3 N-(2-(Benzyloxy)ethyl)-3,5-dinitrobenzamide 
• 1374768-63-4 (3aR,5R,6S,7R,7aR)-5-(acetoxymethyl)-2-(2-(benzyloxy)ethylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diyl diacetate 
• 1374768-64-5 (3aR,5R,6S,7R,7aR)-2-(2-(benzyloxy)ethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diol 
• 1374768-65-6 tert-butyl 2-(benzyloxy)ethyl((3aR,5R,6S,7R,7aR)-6,7-dihydroxy-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-2-yl)carbamate 
• 1374768-66-7 tert-butyl 2-(benzyloxy)ethyl((3aR,5R,6S,7R,7aR)-5-((tert-butyldimethylsilyloxy)methyl)-6,7-dihydroxy-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-2-yl)carbamate 
• 1374768-67-8 tert-butyl 2-(benzyloxy)ethyl((3aR,5R,6S,7R,7aR)-5-((tert-butyldimethylsilyloxy)methyl)-6,7-bis(4-methoxybenzyloxy)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-2-yl)carbamate 
• 1374768-68-9 tert-butyl 2-(benzyloxy)ethyl((3aR,5R,6S,7R,7aR)-5-(hydroxymethyl)-6,7-bis(4-methoxybenzyloxy)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-2-yl)carbamate 
• 1374768-69-0 C₃₇H₄₄N₂O₉S 
• 1374768-70-3 tert-butyl 2-(benzyloxy)ethyl((3aR,5R,6S,7R,7aR)-5-(1-hydroxyethyl)-6,7-bis(4-methoxybenzyloxy)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-2-yl)carbamate 
• 1374768-71-4 tert-butyl 2-(benzyloxy)ethyl((3aR,5R,6S,7R,7aR)-5-(1-hydroxyethyl)-6,7-bis(4-methoxybenzyloxy)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazol-2-yl)carbamate 

Relevant academic research and scientific papers

Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides

We report herein the design and synthesis of a series of novel 5-halogenated-7-azaindolin-2-one derivatives containing a 2,4-dimethylpyrrole moiety. Nine target compounds with ≥70% inhibition against MCF-7 at 30 μM were further evaluated for their in vitro antitumor activity against seven human cancer cell lines by SRB assay. Results reveal that some compounds have potent antitumor activity, and the most active 13c7 (IC50s: 4.49-15.39 μM) was found to be more active than Sunitinib (IC50s: 4.70->30 μM) against all of the tested cancer cell lines.

PYRANO[3,2-D]THIAZOL DERIVATIVES AND USES THEREOF AS SELECTIVE GLYCOSIDASE INHIBITORS

Pyrano[3,2-d]thiazol derivatives of formula (I) for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds are disclosed. Methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc are also provided.

SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF

The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.

Anti-infective compounds

The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.

Di-p-nitrobenzyl azodicarboxylate (DNAD): An alternative azo-reagent for the Mitsunobu reaction

Di-p-nitrobenzyl azodicarboxylate is prepared in 83.6% yield in two steps as a bright yellow solid, which can be used as an azo-reagent in the Mitsunobu reaction. When a chiral secondary alcohol was used, sufficient configurational inversion of alcohol occurred under Mitsunobu conditions. That the hydrazine produced from DNAD is semisoluble in some solvents such as THF and CH 2Cl2 makes it separated easily from the reaction mixture just via filtration. Then the recovered hydrazine compound can be re-exposed to oxidant to produce DNAD. Because DNAD is more stable than DIAD at ambient temperatures and allows easy separation, it is a good alternative azo-reagent for the Mitsunobu reaction.

Dicyclopentyl azodicarboxylate (DCpAD): A new alternative azo-reagent for the Mitsunobu reaction

Dicyclopentyl azodicarboxylate is introduced as a new azo-reagent which can be conveniently prepared in two steps and be used in the Mitsunobu reaction. Though there are no distinct difference of reactivity between DCpAD and DEAD, the former is a more preferable azo-reagent for its stability.