摘要:
The invention relates to novel 1-(4-R.sub.1 O-phenyl)-2-(4-R.sub.2 -phenyl)-6-R.sub.3 -1,2,3,4-tetrahydroquinolines having antifertility and hypocholesterolemic activities, to their preparation, and to novel intermediates therefor.
摘要:
3-(4 OR 3-Pyridinyl)-2-cyclohexen-1-ones (I) and their oxime derivatives are useful in preparing (3-aminophenyl)-pyridines, in turn, useful in preparing known antibacterial agents. Also shown is the preparation of I by starting with the reaction of methyl vinyl ketone with either 1-(pyridinyl)-1-(lower-tertiary-amino)-ethylene (II) or lower-alkyl 3-(pyridinyl)-3-oxopropanoate. Also shown is the process of converting I to its oxime, acylating the oxime and heating the acylated oxime under acidic conditions to produce N-(lower-acyl)-3-(pyridinyl)-aniline (VII), and hydrolyzing VII under aqueous alkaline conditions to produce the corresponding 3-(pyridinyl)aniline.
摘要:
1'-Sulfonylsteroido[3,2-c]pyrazoles, for example, (5.alpha.,17.alpha.)-1'-(methylsulfonyl)-1'H-pregn-20-yno[3,2-c]pyrazol-17-ol, which are useful as antiandrogenic agents, and processes for preparation, method of use and compositions thereof are disclosed.
摘要:
3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalky- or haloalkyl-1H-indole with an amine.
摘要:
Compounds of the formula ##STR1## where R is hydrogen, methyl, ethyl, propyl, 2-propenyl or 2-propynyl; and R' is hydrogen or fluoro possess anti-inflammatory activity. The compounds where R is H are prepared by reacting a compound of the formula ##STR2## with (1H,3H)-pyrimidine-2,4,5,6-tetrone. The compounds where R is other than hydrogen are prepared by reacting a compound where R is hydrogen with the appropriate alkylating agent.
摘要:
4.alpha.,5.alpha.-Epoxy-3,20-dioxopregnane-2.alpha.,16.alpha.-dicarbonitrile is prepared by decyclizing 4.alpha.,5.alpha.-epoxy-20-oxopregn-2-eno-[2,3-d]isoxazole-16.alpha.-carbonitrile with strong base and is useful as an inhibitor of mineralocorticoid production and/or action without concomitant glucocorticoid inhibition in primates.
摘要:
1-R.sub.1 -4-R.sub.4 -.alpha.,.alpha.,2,5-Tetramethylpyrrole-3-acetamides, useful as anti-secretory and anti-ulcer agents, are prepared by hydrolysis, in the presence of a dilute mineral acid, of a corresponding 1-R.sub.1 -4-R.sub.4 -.alpha.,.alpha.,2,5-tetramethylpyrrole-3-acetonitrile.
摘要:
2,4,5,6-Tetrahydrocyclopenta[c]pyrrole-4-carboxamide and 4-thiocarboxamide derivatives useful as antisecretory and anti-ulcer agents are prepared by hydrolysis or thiohydrolysis of the corresponding 2,4,5,6-tetrahydrocyclopenta[c]pyrrole-4-carbonitriles or, in the case of the thiocarboxamides, by reaction of the 4-carboxamide with phosphorus pentasulfide.
摘要:
5-Ethenyl-4,4a,7,8-tetrahydro-4a-methyl-2(3H)-naphthalenone, an intermediate useful in the total synthesis of steroids, is prepared by dehydrohalogenation of 5-(2-bromoethylidene)-2(3H)-4a-methyl-4,4a,5,6,7,8-hexahydronaphthalen-2-one by a pyrolytic procedure or by means of dehydrohalogenating agents, for example, a mixture of lithium bromide and lithium carbonate.