摘要:
THIS INVENTION RELATES TO W-AMINOALKOXY SUBSTITUTED TERPHENYLS AND N-OXIDES THEREOF USEFUL AS HYPOLIPIDEMICS, AND TO PROCESSES FOR PREPARATION OF SUCH COMPOUNDS, INVOLVING KEY INTERMEDIATES WHICH INCLUDE, FOR EXAMPLE: (1) SUBSTITUTED TERCYCLIC-OLS, OR (2) P-(W - AMINOALKOXY)PHENYL DERIVATIVES OF VARIOUS COMPOUNDS WHICH ARE, FOR EXAMPLE, CYCLO-SUBSTITUTED -2-CYCLOHEXEN-1-OLS, CYCLO-SUBSTITUTED -CYCLOHEXENES OR CYCLOHEXEN-DIENES, OR (3) A-(M-TERPHENYL4-YLOXY) LOWER ALIPHATIC MONOCARBOCYCLIC ACIDS.
摘要:
3-Hydroxy-3-(substituted-aminoalkyl)-3,4-dihydro-2H-1,5benzodioxepin products are described that exhibit Beta adrenergic stimulating properties and are therefore suitable for use as broncho-dilating agents. The products are prepared essentially by four principal routes from 3-oxo-3,4-dihydro-2H1,5-benzodioxepins. By one route the 3-oxobenzodioxepin is treated with a nitroalkane to give a 3-hydroxy-3-nitroalkylbenzodioxepin the nitro group of which is reduced to an amine and the resulting compound reacted with an aldehyde or ketone under hydrogenating conditions to introduce the desired substituent into the amino function. By a second route the 3-oxobenzodioxepin is reacted with an alkali metal nitrile to form the cyanhydrin which upon reduction forms the 3-hydroxy-3-aminoalkylbenzodioxepin that can be treated with a ketone or aldehyde to give the desired products or can be reacted with sodium nitrite or other agent to form a 3-spiro-benzodioxepin-2''-oxirane which upon reaction with an amine provides the desired product. The 3spiro-benzodioxepin-2''-oxirane also can be obtained by treatment of the 3-oxo-benzodioxepin with a sulfurylide. A fourth method involves forming a benzodioxepin-3-spiro-5''-oxazolidin-2''-one which upon treatment with dilute alkali gives the desired 3hydroxy-3-(substituted aminoalkyl)-3,4-dihydro-2H-1,5benzodioxepin. The intermediate oxazolidinone compounds can be treated if desired with various agents to attach substituents on the benzenoid moiety of the starting substance. These oxazolidinones exhibit Beta -stimulating and skeletal muscle relaxant properties.
摘要:
NEW (2-HYDROXYHEXAFLUORO-2-PROPYL) BENZ-SUBSTITUTED BENZOHETEROCYCLIC NITROGEN COMPOUNDS USEFUL IN THE PREPARATION OF BENZOHETEROCYCLIC NITROGEN COMPOUND CARBOXYLIC ACIDS AND AS HYPOTENSIVE AGENTS, AND NEW (2-HYDROXYHEXAFLUORO-2-PROPYL)-3,4-DIAMINOBENZENE PRECURSOR FOR SUCH COMPOUNDS.