79545-12-3

Upstream product

• 79545-11-2 4-amino-3-nitrobenzyl cyanide 

Downstream Products

• 25789-73-5 1,2-diamino-4-carbamoylmethylbenzene 
• 132261-04-2 (6R,7R)-3-Acetoxymethyl-7-(5-cyanomethyl-1H-benzoimidazol-2-ylamino)-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid benzhydryl ester 

Relevant academic research and scientific papers

Synthesis and structure-activity relationship of new cephalosporins with amino heterocycles at C-7. Dependence of the antibacterial spectrum and β-lactamase stability on the pK(a) of the C-7 heterocycle

Cephalosporins with new aminobenzimidazole and aminoimidazoline heterocycles at C-7 have been synthesized starting with versatile C-7 isocyanide dihalide synthons. The aminobenzimidazoles have a broad spectrum of antibacterial activity, including Gram-positive and Gram-negative organisms, but possess limited β-lactamase stability. In contrast, the aminoimidazolines have a narrow spectrum of antibacterial activity, limited to Gram-negative strains only, but possess outstanding β-lactamase stability. Structure-activity relationships are discussed in terms of their dependence on the pK(a) of the C-7 amino heterocycle, basic C-7 residues giving cephalosporins with exceptional β-lactamase stability.

Cephalosporin derivatives

A compound of the formula I: STR1 in which R1 is any C-3 substituent from antibacterially-active cephalosporins; R2 is any C-4 substituent from antibacterially-active cephalosporins; R3 is H, hydroxy, amino, 1-6C alkyl, 1-