摘要:
1-Oxo-1H-naphtho [ 2,1-b] pyran derivatives, such as, for instance, 1-oxo-3-(N-methyl-N-ethyl) amino-1H-naphtho [2,1-b] pyran, are disclosed, as well as pharmaceutical compositions containing same and the method of treating depression by administering such compositions.These compounds are active on the central nervous system, and therefore function as antidepressive agents.
摘要:
A multi-step, stereospecific total synthesis of steroids utilizing intermediates having a cyanoalkyl A-ring precursor is disclosed. The initial starting materials for this process are the relatively inexpensive and commercially available reagents .gamma.-butyrolactone and sodium cyanide. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly 19-norsteroids. It is a feature of this process that conditions employed during the multiple step synthesis are selected so as to retain the normally labile nitrile group even during hydrogenation and hydrolysis steps. In this manner, it is possible to employ the nitrile group as an A-ring precursor without resorting to protective groups as was heretofore found necessary in previous steroid total synthesis processes.
摘要:
Novel polycyclic gamma-pyrone derivatives having a carboxaldehyde group on the 3-position and optionally substituted on the 5, 6, 7, 8, 9 or 10 positions with a hydroxy, lower alkyl or lower alkoxy group are disclosed, as well as the corresponding N-substituted, formyl imine derivatives thereof. These compounds, and pharmaceutical compositions containing these compounds, are useful for the treatment of allergic conditions and for the treatment of hyperacidity.
摘要:
This invention relates to protonated compounds of the formula: ##SPC1##Wherein A is a radical selected from ##SPC2##X represents the atoms necessary to complete a ring-closing moiety selected from phthalide and naphthalide; and Z is an anion derived from a protic acid. These compounds are useful as intermediates in the preparation of phthalide and naphthalide indicator dyes.
摘要:
A process for the production of partially saturated gamma-pyrones of the general formula I: ##SPC1##wherein R represents hydrogen, hydroxy, lower alkyl, or lower alkoxy and n represents 1 or 2, by reacting a suitably substituted tetralone (IIa) or indanone (IIb) with a boron trifluoride compound and acetic anhydride to obtain intermediate boron complexes III, which are reacted with a Vilsmeier reagent prepared from phosphorus oxychloride and dimethylformamide to obtain the partially saturated gamma-pyrones of formula I. The gamma-pyrones I have anti-allergy and anti-secretory activity.
摘要:
This invention relates to a process of preparing phthalein indicator dyes including phthalides and naphthalides derived from certain hydroxy-substituted carbocyclic aryl compounds, such as phenols, and from certain N-heterocyclic aryl compounds, such as indoles, and to a process of preparing novel intermediates useful therein. According to the present invention, the selected carbocyclic compound or the selected N-heterocyclic compound is reacted with phthalaldehydic or naphthalaldehydic acid to form the corresponding (na)phthalidyl adduct which is treated with an oxidizing agent to yield the subject intermediates. To prepare the indicator dye, the intermediate, i.e., the oxidation product thus obtained is then reacted with a carbocyclic or heterocyclic aryl compound to yield the corresponding indicator dye. The oxidation products comprising the novel intermediates of the present invention may be dehydro or hydrated (na)phthalidyl adducts.
摘要:
Process for producing isochromans having the structure:
WHEREIN R1 and R2 are each (i) separately selected from the group consisting of hydrogen, lower alkoxyl, lower alkyl, and, (ii) taken together, selected from the group consisting of benzo, cyclopentano, cyclohexano, naphtho, monoalkyl cyclopentano, polyalkyl cyclopentano, monoalkyl cyclohexano and polyalkyl cyclohexano, and R3 and R4 are the same or different and are selected from the group consisting of hydrogen and lower alkyl comprising the steps of intimately admixing: A. An alkanol having the structure:
B. An acetal having the structure:
(wherein R5 and R6 are the same or different alkyl); and C. A protonic acid selected from the group consisting of ptoluene sulfonic acid and phosphoric acid. AND HEATING THE RESULTING MIXTURE FOR A PERIOD OF TIME WHEREBY A SUBSTANTIAL AMOUNT OF THE ISOCHROMAN HAVING THE ABOVE STRUCTURE IS FORMED.
摘要:
Stereo-specific total synthesis of steroidal materials. 7Substituted 3-oxo-1-heptenes or variants thereof are reacted with 2-alkylcycloalkane-1,3-diones yielding 3-substituted 6a Beta alkyl-cyclopenta (f) (l) benzopyrans or naphtho (2,1-b) pyrans. These are then subjected to a selective catalytic hydrogenation followed by an introduction of a hydroxy, alkoxy or acyloxy group at the 4a-position to produce a 3-substituted 6a, Beta , 4ahydroxy, alkoxy or acyloxy perhydrocyclopenta (f) (1) benzopyran or perhydro-naphtho (2,1-b) pyran. These latter compounds are then converted into 4- or 5-(3-oxoalkyl)perhydroindene-5-ones or perhydronaphthalene-6-ones which in turn can be converted to known steroidal materials by known methods.
摘要:
CARBOXY SUBSTITUTED 1-NAPHTHOL NAPHTHALIDE INDICATOR DYES ARE PREPARED BY REACTING A 2-CARBOXY-1-NAPHTHOL AND A 3-ACYLOXY -3-(3''-LOWER CARBOALKOXY-4''-HYDROXY-1''-NAPHTHYL)NAPHTHALIDE IN THE PRESENCE OF A CATALYST HAVEING A HIGH DIPLOE MOMENT TO FORM THE CORRESPONDING DYE PECURSOR WHICH IS THEN HYDROLYZED TO YIELD THE CORRESPONDING INDICATOR DYE PRODUCT.