32864-11-2

Upstream product

• 5417-17-4 2-chloro-3,4-dimethoxybenzaldehyde 
• 37687-57-3 2-chloro-3-hydroxy-4-methoxybenzaldehyde 
• 73894-43-6 6-Bromo-7,8-dimethoxy-1-phenyl-3-trifluoro-acetyl-2,3,4,5-tetrahydro-1H-3-benzazepine 
• 621-59-0 isovanillin 

Downstream Products

• 37687-59-5 3,4-dibenzyloxy-2-chlorobenzaldehyde 
• 110038-97-6 4-Chloro-N-<2-hydroxy-2-(4-methoxyphenyl)ethyl>-1,3-benzodioxole-5-acetamide 
• 110038-81-8 6-Chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-(4-methoxyphenyl)-1H-3-benzazepine hydrochloride 
• 110039-00-4 α-<<<2-4-(4-Chloro-1,3-benzodioxol-5-yl)ethyl>amino>methyl>-4-methoxybenzenemethanol hydrochloride 
• 110039-03-7 4-Chloro-6,7,8,9-tetrahydro-9-(4-methoxyphenyl)-5H-1,3-dioxolo<4,5-h><3>-benzazepine hydrochloride 
• 959088-94-9 2-Amino-1-(3,4-bis-benzyloxy-2-chloro-phenyl)-ethanol 
• 101969-79-3 2-chloro-noradrenaline 

Relevant academic research and scientific papers

Preparation method for removing aromatic methyl ether and methyl

The invention discloses a method for removing aromatic methyl ether and methyl in synthesis of a key intermediate 2-chloro-3, 4-dihydroxybenzaldehyde of cefdinir, and belongs to the field of synthesisof medical intermediates. The method comprises the foll

Preparation method of cephalosporin side chain

The invention provides a preparation method of a cephalosporin side chain. The method comprises the following steps of 2 - chlorine -3 and 4 -methoxybenzaldehyde as raw materials; and under the catalysis of a Lewis acid or base, 2 - chlorine -3 and 4 -dihydroxybenzaldehyde are removed. The hydroxyl group is then protected. Alkylation of aldehyde groups followed by amidation with 1 - (2 - aminoethyl) pyrrolidine gives 3 -position side chains of the cephalosporin. The method uses a novel starting material, is subjected to demethylation, protecting hydroxyl group, oxidizing aldehyde group and amidation to form a four-step reaction. The method is environmentally friendly, easily available in raw materials, simple and convenient to operate, high in product yield and purity, low in cost and easy for industrial production.

Design, synthesis and biological evaluation of C(4) substituted monobactams as antibacterial agents against multidrug-resistant Gram-negative bacteria

A series of novel pyridone conjugated monobactams with various substituents at the (4) position were synthesized and evaluated for their antibacterial activities against a panel of multidrug-resistant (MDR) Gram-negative bacteria in vitro. Compounds 46d, 54 and 75e displayed good to moderate activities against P. aeruginosa, among which the activity of 75e against P. aeruginosa was comparable to that of BAL30072 under iron limitation condition. Compounds 35, 46d, 54, 56a, 56c and 56d exhibited good to excellent antibacterial activities against E. coli and K. pneumoniae, which were comparable or superior to that of BAL30072. In vitro liver microsomal stability was further evaluated and the results manifested that Compounds 35, 46d and 54 were metabolically stable in human liver microsomes.

Comparative α- and β-adrenoceptor activity of 2- and 6-ring-chlorinated noradrenaline analogues

The α- and β-adrenoceptor activity of the 2- and 6-ring-chlorinated analogues of noradrenaline (norepinephrine) were evaluated in vitro. The 2-chloro-substituted analogue exhibits a far greater affinity for β1-chronotropic receptors than the 6-chloro-substituted analogue, whereas no significant differences are apparent for their α-adrenergic affinities.

6-HALO-7,8-DIHYDROXY-1-PHENYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINES

7,8-Dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines having a halo substituent at the 6-position have potent dopaminergic activity. The 6-chloro congeners are most active.

Method for 6-bromination of 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine compounds

The preparation of 6-bromo-7,8-dimethoxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines is described by direct bromination of the nucleus.

HALOGEN SUBSTITUTED ALPHA-(AMINOALKYL)-3,4-DIHYDROXYBENZYL ALCOHOLS

Halogen substituted α-(aminoalkyl)-3,4-dihydroxybenzyl alcohols having β-adrenergic stimulant activity, particularly as selective bronchodilators. The α-aminomethyl derivatives are prepared by the condensation of an appropriately substituted styrene oxide with a primary amine followed by removal of the ether protective group(s). The α-aminoethyl or α-aminopropyl derivatives are prepared by the condensation of an appropriately substituted α-bromoalkyl phenyl ketone with an N-benzyl secondary amine followed by reduction of the ketone moiety and removal of the ether protective group(s).