81079-95-0

Upstream product

• 123-75-1 pyrrolidine 
• 50-00-0 formaldehyd 
• 103-90-2 4-acetaminophenol 

Downstream Products

• 343935-57-9 2,6-bis(1-pyrrolidinomethyl)-4-ethylaminophenol 
• 5201-88-7 4-<3,5-bis<(N-pyrrolidinyl)methyl>-4-hydroxyanilino>-7-chloroquinoline 
• 85236-51-7 3,5-bis(N-pyrrolidinylmethyl)-4-hydroxyaniline 

Relevant academic research and scientific papers

Pyrido[3,2-b]indol-4-yl-amines - Synthesis and investigation of activity against malaria

Starting with 3-aminoindole-2-carboxylic acid ester 1 the annulated pyrido[3,2-b]indoles 6 and 8 were synthesized as key substances. The 4-chloropyridine derivative 8 reacted with the phenol Mannich bases 11 and the novaldiamine base 13, respectively, to yield the amodiaquine and cycloquine analogues 12 as well as the chloroquine analogue 14. The stability of the compounds 12 and 14 were proven by the half wave potentials measured by differential pulse voltammetry. Compounds 12 and 14 were tested for in vitro antimalarial activity using a chloroquine sensitive and a chloroquine resistant Plasmodium falciparum strain. The highest activity was shown by 12g with IC 50 values of 50 nM and 38 nM, respectively. The in vivo activity of 12g was tested in Plasmodium vinckei infected mice resulting in ED50 values of 22 mg/kg and 26 mg/kg after intraperitoneal and oral administration, respectively.

Microwave-induced Mannich reaction - Synthesis of some Mannich derivatives of p-aminophenol

Mono and bis substituted dialkylamino alkyl-p-aminophenol 3 are prepared by treating paracetamol 1 with formaldehyde and appropriate secondary amines followed by deacetylation using 6 M HCI in unmodified domestic microwave oven in unsealed borosil vessels

Aryl substituted aminomethyl benzene derivatives having antiarrhythmic utility

The present invention relates to new compounds of the formula STR1 wherein X is STR2 wherein R1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y)A is positioned ortho to W and is an aminoloweralkyl having the formula --CH2 NR2 R3 where R2 and R3 are the same or different and may be lower alkyl or R2 and R3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C1 -C10 alkyl, straight or branched C3 -C10 cycloalkyl, straight or branched C2 -C4 alkenyl or straight or branched C2 -C4 alkynyl, or a pharmaceutically acceptable salt thereof. These compounds are useful in the treatment of various cardiac arrhythmias.

Synthesis and Antiarrhythmic and Parasympatholytic Properties of Substituted Phenols. 1. Heteroarylamine Derivatives

Twenty-four structural derivatives of the antiarrhythmic drug changrolin were synthesized and tested for antiarrhythmic and parasympatholytic activities.It was found that while the bis(pyrrolidinylmethyl)phenol pattern of changrolin appeared to be optimal