EurekaMag.com logo
+ Site Statistics
References:
52,725,316
Abstracts:
28,411,598
+ Search Articles
+ Subscribe to Site Feeds
EurekaMag Most Shared ContentMost Shared
EurekaMag PDF Full Text ContentPDF Full Text
+ PDF Full Text
Request PDF Full TextRequest PDF Full Text
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter
Follow on Google+Follow on Google+
Follow on LinkedInFollow on LinkedIn

+ Translate

Primary secondary and tertiary alpha alpha n di substituted alkylamines synthesis and pharmacology






European Journal of Medicinal Chemistry 12(4): 351-359

Primary secondary and tertiary alpha alpha n di substituted alkylamines synthesis and pharmacology

A series of primary secondary and tertiary alkylamines, .alpha.,.alpha.-disubstituted, saturated or unsaturated, were prepared. The 2 most common syntheses were Ritter's reaction on tertiary alkanols and Hofman's degradation reaction on .alpha.,.alpha.:disubstituted alkylamides. The pharmacological study with rats gave clear indication of an antiparkinsonian activity. They showed a common profile characterized by an inhibitory action of the neuroleptic and reserpinic catatonia and a lack of cholinolytic properties. A comparison made between dipropyl-1,1 butylamine and other parkinsonians (L-dopa, apomorphine, amphetamine and particularly amantadine), showed the former to be the most active product.


Accession: 006184566



Related references

Shaw, A.W.; Desolms, S.J.ne, 2001: Asymmetric synthesis of alpha,alpha-diaryl and alpha-aryl-alpha-heteroaryl alkylamines by organometallic additions to N-tert-butanesulfinyl ketimines. Organometallic addition to tert-butanesufinyl ketimines derived from diaryl and aryl-heteroaryl ketones provided the corresponding alpha,alpha-diaryl and alpha-aryl-alpha-heteroaryl alkylamines in good yield with high diastereoselectivity. In many...

Mulinos, M.G.; Disick, S., 1941: The pharmacology of some derivatives of mono alpha secondary furfurylamine and of di-alpha furfuryl tertiary amine. 6 derivatives of [alpha]-furfuryl-amine (methyl, ethyl, n-propyl, n-butyl, n-amyl and phenyl) and 5 derivatives of [alpha]-di-furfuryl-amine (methyl, ethyl, n-propyl- n-butyl and n-amyl) were studied as to toxicity and the effect upon blood pressu...

French, A.N.; Wilson, S.R.; Welch, M.J.; Katzenellenbogen, J.A., 1993: A synthesis of 7 alpha-substituted estradiols: synthesis and biological evaluation of a 7 alpha-pentyl-substituted BODIPY fluorescent conjugate and a fluorine-18-labeled 7 alpha-pentylestradiol analog. In an effort to assist in the preparation of ligands for the study of the estrogen receptor (ER), we have developed a new synthesis of 7 alpha-substituted estradiols. The key step in the synthesis involves a copper-catalyzed, alpha-selective, 1,6-...

Probst, K.C.; Jung, G., 2006: Solid-phase S-3CR generates N-substituted alpha-aminonitriles for the synthesis of alpha-phenyl-alpha-(1-piperazinyl) substituted amino acids. Structurally diverse amino acids were prepared as versatile synthons for combinatorial chemistry. Using an optimized solid-phase synthesis by Strecker-three-component-reaction (S-3CR), two different polymer linker constructs carrying piperazine we...

Ezquerra, J.; Pedregal, C.; Moreno Manas, M.; Pleixats, R.; Roglans, A., 1993: Synthesis of alpha-substituted and alpha,alpha-disubstituted alpha-amino acids by controlled mono- and dialkylation of ethyl N-diphenylmethyleneglycinate. Tetrahedron Letters 34(52): 8535-8538

Suginome H.; Ohue Y.; Orito K., 1987: Synthesis of 16 substituted 17 nor 13 alpha steroids and skeletal rearrangement of 17 nor 5 alpha 13 alpha androstane 16 alpha carbonyl m chlorobenzoyl peroxide. The reaction of 17-nor-5.alpha.,13.alpha.-androstane-16.beta.-carbonyl chloride with m-chloroperbenzoic acid led to a skeletal rearrangement that resulted in an abeo homodinorsteroid identical with one obtained by the reaction of 17-nor-5.alpha.-a...

Bakinovskiń≠, L.V.; Gomtsian, A.R.; Bań≠ramova, N.E.; Kochetkov, N.K., 1985: Synthesis of oligosaccharide fragments of O-specific polysaccharides of Shigella flexneri. III. Synthesis of the tetrasaccharide Glc alpha 1-3Rha alpha 1-2(Glc alpha 1-3)Rha alpha 1-OMe and the pentasaccharide GlcNAc beta 1-2(Glc alpha 1-3)Rha alpha 1-2(Glc alpha 1-3)Rha alpha 1-OMe. Two synthetic schemes to prepare the title branched tetrasaccharide and pentasaccharide are described. These oligosaccharides represent fragments of the O-antigenic polysaccharides of Shigella flexneri serotype 5b.

Spero, D.M.; Kapadia, S.R., 1996: Enantioselective Synthesis of alpha,alpha-Disubstituted Amino Acid Derivatives via Enzymatic Resolution: Preparation of a Thiazolyl-Substituted alpha-Methyl alpha-Benzyl Amine. A new and efficient enantioselective synthesis of the (S)-alpha,alpha-disubstituted phenethylamine 1 via Lipase resolution of the esters 3 and 4 is described. The effect of pH, enzyme load, and solubilizing additives has been studied and optimized...

Pala, G.; Bruzzese, T.; Mantegani, A., 1964: Naphthylacetamides. I. Secondary And Tertiary 1-Naphthylacetamides Substituted And Non-Substituted In The Alpha Position With Alkyl Radicals. Il Farmaco; Edizione Scientifica 19: 235-245

Bejaud M.; Mion L.; Taillades J.; Commeyras A., 1975: The strecker synthesis and related systems part 4 a comparative study of the reactivity of secondary and tertiary alpha amino nitriles in aqueous solutions between ph 10 and 14 hydrolysis of secondary alpha amino nitriles and its importance in the prebiotic formation of natural amino acids. Tetrahedron 31(5): 403-410