- IMPROVED PROCESS FOR THE MANUFACTURE OF R-6-HYDROXY-8-[1-HYDROXY-2-[2-(4-METHOXYPHENYL)-1,1-DIMETHYLETHYLAMINOETHYL]-2H-1,4-BENZOXAZIN-3(4H)-ONE HYDROCHLORIDE
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The present invention provides an improved process for the manufacture (R)-6- hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4- benzoxazin-3(4H)-one, in high purity and high yield, through the use of 1,1-dimethyl-2- (4-met
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- CALCILYTIC COMPOUNDS
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Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.
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- 1-DIPHENYLPHOSPHINYL-2,2-DIMETHYLAZIRIDINE - A NEW PRECURSOR OF α,α-DIMETHYLARYLALKYLAMINES
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The new synthesis of α,α-dimethylarylalkylamines from 1-diphenylphosphinyl-2,2-dimethylaziridine is described.
- Buchowiecki, Wieslaw,Grosman-Zjawiona, Zofia,Zjawiony, Jordan
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p. 1245 - 1248
(2007/10/02)
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- Derivatives related to betaxolol with α- and β-adrenergic activities
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The paper describes the synthesis and the pharmacological evaluation of some derivatives of betaxolol, all with an N-aralkylamine instead of the tertiobutylamine. These compounds have been tested for β1-adrenergic receptor antagonism on guinea pig atria, β2-adrenergic receptor antagonism on guinea pig trachea and α-adrenergic blocking activity on rat aorta. Compound U12 with a marked α-blocking activity and compound R8 with a β1/α ratio = 1 were selected for a haemodynamic study in the dog. The decrease in cardiac work and the diminution of total peripheral resistance exhibited by U12 are consistent with a dual α/β-blocking agent. Finally, structure-activity relationships are discussed.
- Leclerc,Decker,Schwartz
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p. 1357 - 1367
(2007/10/02)
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- Novel benzylalcohol derivative and process for preparing the same
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A benzylalcohol derivative of the formula: STR1 wherein R is hydroxy, benzyloxy, alkoxy of one to 4 carbon atoms or halogen, and Ring A is monomethoxyphenyl, dimethoxyphenyl, trimethoxyphenyl or 3,4-methylenedioxyphenyl is prepared by reducing a compound of the formula: STR2 wherein R' is benzyloxy, alkoxy of one to 4 carbon atoms or halogen, and Ring A is the same as defined above, and when R' is benzyloxy, if required, further subjecting the product to catalytic hydrogenation. The compounds (I) and pharmaceutically acceptable acid addition salts thereof are used as anti-diabetic agents.
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