40105-98-4

Upstream product

• 40105-95-1 4,4-diphenyl-N-benzylpiperidine 
• 541-41-3 chloroformic acid ethyl ester 
• 71-43-2 benzene 
• 63843-83-4 1-benzyl-4-hydroxy-4-phenylpiperidine 
• 3612-20-2 1-phenylmethyl-4-piperidone 
• 29976-53-2 N-ethoxycarbonyl-4-piperidone 

Downstream Products

• 31314-44-0 1-(2-hydroxyethyl)-4,4-diphenylpiperidine 
• 35985-34-3 1-(3-hydroxypropyl)-4,4-diphenylpiperidine 
• 35879-51-7 1-acetonyl-4,4-diphenylpiperidine 
• 31314-37-1 1-ethyl-4,4-diphenylpiperidine 
• 91075-60-4 1-Pivaloyl-4,4-diphenylpiperidin 
• 91075-45-5 1-n-butyl-4,4-diphenylpiperidine 
• 91075-47-7 1-(2-acetoethyl)-4,4-diphenylpiperidine 

Relevant academic research and scientific papers

Dicationic intermediates involving protonated amides: Dual modes of reactivity including the acylation of arenes

Matrix presented. In the Bronsted superacid CF3SO 3H (triflic acid), amides are able to form reactive, dicationic electrophiles. It is shown that these dicationic intermediates participate in two distinctly different types of electrophilic reactions. The protonated amide increases the reactivity of an adjacent electrophilic group, and the protonated amide group itself shows enhanced reactivity arising from an adjacent cationic charge. In the latter case, several types of amides are even capable of reacting with benzene by Friedel-Crafts acylation.

Synthesis, physico-chemical properties and pharmacological screening results of budipine and related 1-alkyl-4,4-diphenylpiperidines

1-Alkyl-4,4-diphenylpiperidines are accessible in a simple manner and with attractive yields by regioselective reaction of certain piperidine derivatives, particularly 3-aroyl-4-aryl-4-hydroxypiperidines, which can be varied widely at the nitrogen atom, with benzene under Friedel-Crafts conditions. The physico-chemical parameters, which are important for the transport and the distribution of a drug in a living system, are discussed for the 1-tert-butyl derivative (13) (budipine) (pK(a), partition coefficient P, saturation concentration c(s), surface activity, protein binding). Rapid absorption of this drug in man is indicated by the size of the permeability coefficient P(M) of the passive transport through artificial phospholipid collodium membranes as well as the invasion curves calculated from P(M). According to pharmacological screening tests, most of the compounds of this class show marked antagonistic activity against experimentally generated pathological states in mice (tremorine and reserpine antagonism) which suggest their potential use in the therapy of Parkinson's disease. 13 has been selected for detailed investigations. Structure-activity analyses did not readily demonstrate the presence of a relationship between the type of alkyl substituent at the piperidine nitrogen atom and the pharmacological screening results obtained.