97760-95-7

Upstream product

• 93129-68-1 4-acetylamino-3-fluoro-benzonitrile 
• 122-85-0 para-acetamidobenzaldehyde 
• 97760-94-6 N-(2-fluoro-4-iodo-phenyl)-acetamide 
• 29632-74-4 2-fluro-4-iodoaniline 
• 348-54-9 2-Fluoroaniline 

Downstream Products

• 97776-40-4 1-(4-Amino-3-fluoro-phenyl)-2-ethylamino-ethanol 
• 56795-45-0 4'-amino-3'-cyano-5'-fluoro-acetophenone 
• 54238-83-4 1-(4-Amino-3-chloro-5-fluoro-phenyl)-2-ethylamino-ethanone 
• 740030-01-7 1-(4-Amino-3-bromo-5-fluoro-phenyl)-2-ethylamino-ethanone 
• 56340-17-1 4'-amino-2-tert-butylamino-3'-fluoro-5'-iodo-acetophenone 
• 783246-62-8 1-(4-Amino-3-bromo-5-fluoro-phenyl)-2-(1,1-dimethyl-propylamino)-ethanone 
• 97776-43-7 1-(4-Amino-3-chloro-5-fluoro-phenyl)-2-ethylamino-ethanol 
• 97776-45-9 1-(4-Amino-3-bromo-5-fluoro-phenyl)-2-ethylamino-ethanol 
• 95656-56-7 1-(4'-Amino-3'-fluoro-5'-iodo-phenyl)-2-tert-butylamino-ethanol 
• 97776-50-6 1-(4'-Amino-3'-bromo-5'-fluoro-phenyl)-2-tert-pentylamino-ethanol 
• 54240-25-4 4'-amino-3'-bromo-2-cyclopropylamino-5'-fluoro-acetophenone 
• 745725-51-3 1-(4-Amino-3-bromo-5-fluoro-phenyl)-2-(2-hydroxy-1,1-dimethyl-ethylamino)-ethanone 
• 56340-21-7 2-Amino-5-(2-ethylamino-acetyl)-3-fluoro-benzonitrile 
• 752925-84-1 1-(4-Amino-3-bromo-5-fluoro-phenyl)-2-isopropylamino-ethanone 

Relevant academic research and scientific papers

PHENYLALKYL AND PYRIDYLALKYL PIPERAZINE DERIVATIVES

This invention relates to compounds of the formula (1) wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.

Halogenated antituberculosis agents

Halogenated derivatives of two synthetic anti-tuberculosis agents, thioacetazone and p-aminosalicylic acid, have been synthesized. In general, the halogenated compound has the structure of Structure I: wherein X1is a halogen and X2is a second halogen or hydrogen, and Y is sulfur or oxygen; or, has the structure of Structure IV: wherein X1is a halogen and X2is a second halogen or hydrogen. Alternatively, the halogenated compounds may be pharmaceutically acceptable salts of these compounds. These halogenated derivatives possess anti-mycobacterial activity and are particularly useful for the treatment of Mycobacterium tuberculosis infections. In particular, fluorinated analogs of thioacetazone and p-amino-salicylic acid have been synthesized for use as anti-tuberculosis therapeutic agents either alone or in combination with other conventional anti-tuberculosis therapeutic agents.

Synthesis of further amino-halogen-substituted phenyl-aminoethanols

Starting from clenbuterol as a lead structure, new 4-amino-phenyl-aminoethanol analogues have been synthesized by different approaches. In these compounds one or both of the chlorine atoms of clenbuterol are replaced by other residues. This has led to compounds with high intrinsic β2-mimetic and/or β1-blocking activities. 1-(4-Amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butylamino-ethanol hydrochloride (mabuterol) has been selected for clinical development. A detailed description is also given of the syntheses of new intermediate acetophenone derivatives as well as of the resolution of mabuterol into its enantiomers.