5978-34-7Relevant academic research and scientific papers
Dopamine-beta-hydroxylase inhibitors
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, (2008/06/13)
Dopamine-β-hydroxylase inhibitors of structure: Pharmaceutical compositions containing them and their use in methods of lowering blood pressure in mammals.
SELECTIVE DESULFURIZATION OF 1,3-DITHIANES, -OXATHIOLANES AND -THIAZOLIDINES BY TRIBUTYLTIN HYDRIDE
Schmidt, K.,O'Neal, S.,Chan, T.C.,Alexis, C.P.,Uribe, J.M.,et al.
, p. 7301 - 7304 (2007/10/02)
Selective desulfurization of 2-alkyl-1,3-dithianes, -oxathiolanes, or -thiazolidines 1 with one equivalent of tri-n-butyltin hydride yields acyclic compounds R1R2CHX(CH2)nSSnBu3 (X=S,O,NH; n=2,3), (2) which can be destannylated to the corresponding mercaptans 3.
Structure-Activity Relationships among Di- and Tetramine Disulfides Related to Benextramine
Alvarez, M.,Granados, R.,Mauleon, D.,Rosell, G.,Salas, M.,et al.
, p. 1186 - 1193 (2007/10/02)
The synthesis and irreversible α-blocking activity in the rat vas deferens of a series of tetra- and diamine disulfides 2-38, structural analogues of benextramine (BHC), are described. All compounds containing a central cystamine moiety displayed an irreversible α-adrenergic blockade at concentrations ranging from 10-4 to 6*10-6 M. Potency was increased in cystamines N,N'-disubstituted with 6-aminohexyl groups, especially when the outer nitrogen atoms bear arylalkyl substituents or are enclosed in a ring. However, N,N,N',N'-tetrasubstituted cystamines were poor blockers. Structural specificity in the outer portion of the tetramine disulfide is low, since many types of substituents gave rise to potent α-blockers. Even replacement of the outer amines with nonbasic ethers or amides was observed to maintain irreversible α-blockade.
Syntheses de β-sultames (thiazetidines-1,2 dioxyde-1,1)
Champseix, A.,Chanet, J.,Etienne, A.,Berre, A. Lemasson, J. C.,Napierala, C.,Vessiere, R.
, p. 463 - 472 (2007/10/02)
β-sultams (1,2-thiazetidine-1,1-dioxides) are easily prepared by 1-halogensulphonyl-2-aminoalkane cyclisation. Two processes based upon this principle have permitted the preparation of many variously N and C-substituted β-sultams. 1) In the first method 1-chlorosulphonyl-2-aminoalkane hydrochlorides, prepared from taurines or β-aminothiols, cyclised in the presence of base. 2) The second process involves the spontaneous cyclisation of 1-fluorosulphonyl-2-aminoalkanes prepared Michael addition of primary amines to 1-fluorosulphonylethene.
