Abstract: The present invention is directed to radiolabeled N-substituted-6-iodo-3,14-dihydroxy-4,5.alpha.-epoxymorphinans, intermediates for producing the same, and a process for the preparation and methods of detecting opioid receptors.The radioimaging agent of the present invention has the following formula: ##STR1## wherein I is selected from the group consisting of .sup.123 I and .sup.125 I; and where R is alkyl, cycloalkylloweralkyl or allyl.

Abstract: This invention is in the field of clinical neurology and relates specifically to compounds, compositions and methods for treatment of patients with generalized epilepsy or partial (symptomatic) epilepsy using compounds of the formula: ##STR1## This invention also relates to compounds, compositions and methods of treatment for drug craving in patients addicted to cocaine.

Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders and convulsions. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms, and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.

Abstract: A process for preparing hydroxy-substituted-4-alkoxyphenylacetic acids by reacting a 4-alkoxyphenylacetic acid with bromine and then treating the brominated acid with a strong base and a copper salt to form the desired hydroxy-substituted-4-alkoxyphenylacetic acid.

Abstract: Fluorinated derivatives 3,14-dihydroxy-4,5.alpha.-epoxy-6.beta.-fluoro-17-methylmorphinan ("fluorooxymorphone"; FOXY, compound 10) and 17-cyclopropylmethyl-3,14-dihydroxy-4,5.alpha.-epoxy-6.beta.-fluoromorphin an (CYCLOFOXY, compound 18) are prepared based upon the structures of the potent opioid agonist oxymorphone 4 and the antagonist naltrexone 11, respectively. Fluorine was introduced in the final stages of synthesis by a facile nucleophilic displacement with fluoride ion of the 6.alpha.-triflate functions in 8 and 16. The synthetic procedures were suitable for the production of the corresponding positron emitting .sup.18 F-labeled analogs .sup.18 F-FOXY and .sup.18 F-CYCLOFOXY, which are useful for in vivo studies of the opioid receptor system using positron emission transaxial tomography. In addition, the tritiation of FOXY (10) to high specific activity is noted.

Abstract: A derivative of phencyclidine (1) bearing an isothiocyanate moiety on the meta position of the aromatic ring (3; Metaphit as methanesulfonate and HCl salt) has been synthesized and identified as a rapid and specific site-directed acylating agent of the [.sup.3 H]-phencyclidine binding site in rat brain homogenates. Additional related compounds to Metaphit are Thiophit (oxalate salt), Ethylphit (HCl salt), and Isopropylphit (HCl salt).

Abstract: In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically active enantiomers can serve as important intermediates for both natural and unnatural opioids. As a special function of this invention, certain of the derivatives, namely 4'-6' and 7'-9', may be hydrogenated to 1'-3' derivative by asymmetric reduction either of the catalytic or chemical type.

Abstract: There is disclosed herewith a method of producing morphinan compounds by total synthesis which incorporates utilization of N-cycloalkylcarbonyl compounds, which show certain advantages over the prior art which has been previously expressed in U.S. Pat. No. 4,368,326.

Abstract: A derivative of phencyclidine (1) bearing an isothiocyanate moiety of the meta position of the aromatic ring (2; Metaphit) has been synthesized and identified as a rapid and specific site-directed acylating agent of the [.sup.3 H]-phencyclidine binding site in rat brain homogenates.

Abstract: In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically active enantiomers can serve as important intermediates for both natural and unnatural opioids.

Abstract: This invention relates to compounds which may be described as the unnatural enantiomers of morphine agonists and antagonists, which are useful as antitussives. The synthesis utilized is capable of producing all of the unnatural enantiomers of medically important opium derivatives of the morphinan type, including thebaine.

Abstract: In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically active enantiomers can serve as important intermediates for both natural and unnatural opioids.

Abstract: A method of producing morphinan compounds which incorporates double advantages over the prior art, such as the utilization of .beta.,.gamma.-unsaturated ketones in place of the .alpha.,.beta.-unsaturated ketones previously used. Additionally, in the step where .beta.,.gamma.-unsaturated bromoketones (13 or 14) proceed to 1-bromo-N-formylnordihydrothebainone (morphinan) (17) there are utilized super acids, such as trifluoromethane sulfonic, trifluoroethane sulfonic and mixtures thereof, and also antimony pentafluoride and mixtures of hydrogen fluoride and antimony pentafluoride. Super acid works, whereas the prior art shows that cyclization in the presence of acids, even strong acids, such as sulfuric, phosphoric, do not work.

Abstract: Tricyclic aromatic compounds of the formula ##STR1## including those wherein: (A) R.sub.1 is H, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;(b) R.sub.1 is acetyl, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;(c) R.sub.1 and R.sub.3 are methyl and R.sub.2 is carbomethoxy;(d) R.sub.1, R.sub.2, and R.sub.3 are hydrogen; and(e) R.sub.1 and R.sub.3 are methyl and R.sub.2 is hydrogenAre intermediates for the total synthesis of steroids.

Abstract: Tricyclic aromatic compounds of the formula ##STR1## including those wherein: (A) R.sub.1 is H, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;(b) R.sub.1 is acetyl, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;(c) R.sub.1 and R.sub.3 are methyl and R.sub.2 is carbomethoxy;(d) R.sub.1, R.sub.2, and R.sub.3 are hydrogen; and(e) R.sub.1 and R.sub.3 are methyl and R.sub.2 is hydrogenAre intermediates for the total synthesis of steroids.

Abstract: Tricyclic aromatic compounds of the formula ##STR1## including those wherein: A. R.sub.1 is H, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;B. R.sub.1 is acetyl, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;C. R.sub.1 and R.sub.3 are methyl and R.sub.2 is carbomethoxy;D. R.sub.1, R.sub.2, and R.sub.3 are hydrogen; andE. R.sub.1 and R.sub.3 are methyl and R.sub.2 is hydrogenAre intermediates for the total synthesis of steroids.