75271-94-2

Upstream product

• 6342-56-9 Pyruvic aldehyde dimethyl acetal 
• 131120-05-3 3,3-dimethoxy-2-<(trimethylsilyl)oxy>-1-propene 
• 53250-16-1 cyclohexyl-(2,2-dimethoxy-1-methyl-ethylidene)-amine 

Downstream Products

• 83053-37-6 4-Dimethoxymethyl-2-(o-hydroxyphenyl)-thiazol 
• 1429373-07-8 3,3-dimethoxy-2-oxopropyl-1-(triphenylphosphoranylidene) 
• 623906-29-6 2-formyl-6,7-dihydro-5H-cyclopenta[d]imidazo[2,1-b][1,3]thiazole 
• 1000701-69-8 tert-butyl 2-(benzyloxycarbonylamino)-4-dimethoxymethyl-1H-imidazol-1-carboxylate 

Relevant academic research and scientific papers

2-Aminoimidazole facilitates efficient gene delivery in a low molecular weight poly(amidoamine) dendrimer

Functional groups have shown great potential in gene delivery. However, a number of the reported functional groups can only overcome one certain physiological barrier, resulting in limited transfection efficiencies. Based on the structure-activity relationships of both imidazolyl and guanidyl, we designed a novel multifunctional group, 2-aminoimidazole (AM), for gene delivery. On modifying with the AM group, the transfection efficiency of low molecular weight poly(amidoamine) (G2) was 200 times greater than the parent dendrimer in vitro. In contrast, the transfection efficiency of G2 showed a decreasing trend when it was grafted with imidazole. Assays revealed that the AM group played multiple roles in gene delivery, including condensing DNA into monodisperse nanoparticles of 80-90 nm in diameter, achieving nearly ten times higher cellular-uptake efficacy, and enhancing the abilities of endosome/lysosome escape and nuclear localization. What's more, AM showed low toxicity. These results demonstrate that the AM group could be a promising tool in non-viral gene delivery.

Synthesis of Islatravir Enabled by a Catalytic, Enantioselective Alkynylation of a Ketone

The synthesis of the potent anti-HIV investigational treatment islatravir is described. The key step in this synthesis is a highly enantioselective catalytic asymmetric alkynylation of a ketone. This reaction is a rare example of the asymmetric addition o

Synthesis and biological evaluation of piperazine derivatives as novel isoform selective voltage-gated sodium (Nav) 1.3 channel modulators

Sponges of the genus Agelas produce compounds that modulate the activity of voltage-gated sodium ion channels and contribute novel scaffolds for the development of compounds with activity against a plethora of biological targets. In particular, clathrodin and dibromosceptrin were reported to decrease the average maximum amplitude of inward sodium currents in isolated chick embryo sympathetic ganglia cells; we envisaged these compounds as a starting point to design novel Nav channel modulators. This endeavor was part of our long-term goal of designing a comprehensive library of Agelas alkaloid analogs that would cover a broader chemical space and allow us to examine the activity of such compounds on Nav channels. Our series of compounds was designed by maintaining the terminal structural features found in clathrodin while rigidizing the central part of the molecule and replacing the 3-aminopropene linker with a 4-methylenepiperazine moiety. Synthesised compounds were screened for inhibitory action against the human voltage-gated sodium channel isoforms Nav 1.3, Nav 1.4, cardiac Nav 1.5, and Nav 1.7 using an automated patch clamp electrophysiology technique. The results demonstrate that we have obtained a series of compounds with a modest but selective inhibitory activity against the Nav 1.3 channel isoform. The most potent compound showed selective activity against the Nav 1.3 channel isoform with an IC50 of 19 μM and is a suitable starting point for further development of selective Nav 1.3 channel modulators. Such compounds could prove to be beneficial as a pharmacological tool towards the development of novel therapeutically useful compounds in the treatment of pain.

Synthetic bacteriochlorins with integral spiro-piperidine motifs

A new molecular design incorporates a spiro-piperidine unit in each pyrroline ring of synthetic bacteriochlorins, thereby (1) replacing the previous geminal dimethyl group with a functionally equivalent motif to suppress adventitious dehydrogenation, (2)

A novel synthesis of the 2-amino-1H-imidazol-4-carbaldehyde derivatives and its application to the efficient synthesis of 2-aminoimidazole alkaloids, oroidin, hymenidin, dispacamide, monobromodispacamide, and ageladine A

A novel synthesis of 2-amino-1H-imidazol-4-carbaldehyde derivatives was achieved by the reaction of tert-butoxycarbonylguanidine with 3-bromo-1,1-dimethoxypropan-2-one as a key step. The usefulness of the derivatives as building blocks was proved by accomplishing the efficient synthesis of the representative 2-aminoimidazole alkaloids, oroidin, hymenidin, dispacamide, monobromodispacamide, and ageladine A.

A practical route to pyrazines and quinoxalines, and an unusual synthesis of benzimidazoles

1,2-Dicarbonyl compounds can be accessed by a radical addition-transfer of xanthates and used for the synthesis of pyrazines and quinoxalines, as well as in an unusual approach to benzimidazoles.

Process for preparing beta-lactamase inhibitors

The present invention relates to processes for preparing β-alkylidene penem derivatives that can be important as broad spectrum β-lactamase inhibitors and anti-bacterial agents.

2-Phenylthiazole Derivatives from Pseudomonas cepacia

From the culture medium of Pseudomonas cepacia 2-(o-hydroxyphenyl)-thiazol and its 4-carbaldehyd and 4-carboxylic acid derivatives (aeruginoic acid) could be isolated.Their structures were elucidated and confirmed by synthesis. - Key words: Phenylthiazols, Bacterial Metabolites, Pseudomonas cepacia, Mass Spectra