Abstract: Derivatives of 9-deazaguanine of the formula I: are prepared by reacting an aldehyde or ketone of the formula II: with a dialkylaminomalonate to produce an enamine. The enamine is then reacted with a base to produce a pyrrole represented by the formula: The pyrrole is reacted with a compound represented by the formula R3OC(O)N?C(Z)NHC(O)OR3 or a derivative of carbamimidoic acid to provide a protected guanidine compound. The guanidine compound is converted to the desired deazaguanine by reaction with 1) trifluoracetic acid or 2) C1-C4 alkoxide or alkali metal or alkaline earth metal hydroxide followed by neutralization with an acid.

Abstract: Derivatives of 9-deazaguanine are prepared by reacting an aldehyde or ketone with a dialkylaminomalonate to form the corresponding enamine. The enamine is then reacted with a base to form a cyclic pyrrole. The cyclic pyrrole is reacted with an urea compound or a derivative of carbamimidoic acid to provide a protected guanidino compound. The guanidino is converted to the desired 9-deazaguanine derivative by reacting with trifluoracetic acid or with an alkoxide or hydroxide followed by neutralization with an acid.

Abstract: The invention relates to methods for preparing substituted cyclopentene compounds, their intermediates and use as neuraminidase inhibitors.

Abstract: A process for preparing isoflurane (1-chloro-2,2,2-trifluoroethyl difluoromethyl ether) by reacting PFE (2,2,2-trifluoroethyl difluoromethyl ether) with chlorine in the presence of ultraviolet light and added water, at a low temperature and/or at a high conversion.

Abstract: Derivatives of 9-deazaguanine are prepared by reacting an aldehyde or ketone with a dialkylaminomalonate to form the corresponding enamine. The enamine is then reacted with a base to form a cyclic pyrrole. The cyclic pyrrole is reacted with an urea compound to provide a protected guanidino compound. The guanidino is converted to the desired 9-deazaguanine derivative by reacting with trifluoracetic acid or with an alkoxide or hydroxide followed by neutralization with an acid.

Abstract: Substituted 8-amino-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines useful in treating mental disorders and which have activities of prolonged duration are disclosed. Methods for preparing these compounds and methods for their use are also described.

Abstract: Novel compounds including 1-aryl-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofurans such as 1-(4-chlorophenyl)-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofuran, and 1-aryl-1-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dihydroisobenzofurans are disclosed. The corresponding benzo[c]thiophenes, isochromans, and isothiochromans and antifungal pharmaceutical compositions containing same, and methods of using said pharmaceutical compositions to elicit an antifungal response in warm blooded animals having a susceptible antifungal infection are also disclosed.

Abstract: Novel compounds including 1-aryl-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofurans such as 1-(4-chlorophenyl)-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofuran, and 1-aryl-1-(1H-1,2,4-trizazol-1-ylmethyl)-1,3-dihydroisobenzofurans are disclosed. The corresponding benzo[c]thiopenes, isochromans, and isothiochromans and antifungal pharmaceutical compositions containing same, and methods of using said pharmaceutical compositions to elicit an antifungal response in warm blooded animals having a susceptible antifungal infection are also disclosed.

Abstract: A process for the coupling of a chloroperfluoroalkane having a --CFCl.sub.2 moiety which comprises heating the alkane at a temperature of about 150.degree. to 260.degree. C. in the presence of at least about 0.1 times the molar amount each of copper and zinc at a mole ratio of copper:zinc from about 2:1 to 1:2. The product is obtained in relatively high yield and conversion.

Abstract: In the reaction of a 2,2,2-trifluoroethyl halide with ammonia to produce 2,2,2-trifluoroethylamine, the improvement which comprises effecting the reaction with from about 1 to 3 moles of ammonia per mole of the trifluoroethyl halide at a temperature of about 170.degree. to 240.degree. C. and a pressure less than about 300 psig in the presence of a substantially anhydrous inert solvent present in at least about the same molar amount as the trifluoroethyl halide. Advantageously the temperature is from about 200.degree. to 220.degree. C., the pressure is at most about 250 psig, the solvent is N-methylpyrrolidone present in at least about 3 times the molar amount of the trifluoroethyl halide, and the halide is the chloride.

Abstract: 1-Methyl-6-substituted-4-phenyl-quinazolin-2-one-3-oxides and their use as intermediates in the preparation of 3-fluorobenzodiazepines which are useful as tranquilizers, muscle relaxants and sedatives.