Abstract: Analgesic 1,2,3,4-tetrahydroisoquinolines of the formula (1) ##STR1## wherein R.sub.1 and R.sub.2 respectively are hydrogen, hydroxy or alkoxy of 1 to 4 carbon atoms, R.sub.3 and R.sub.4 respectively are hydrogen or alkyl of 1 to 4 carbon atoms, and R.sub.5 is hydroxy, nitro or ##STR2## wherein R.sub.6 and R.sub.7 respectively are hydrogen, alkyl of 1 to 4 carbon atoms or RCO-- wherein R is hydrogen or alkyl of 1 to 4 carbon atoms; pharmaceutically acceptable addition salts thereof with non-toxic acids; analgesic compositions thereof in an inert, pharmaceutical carrier; and methods of preparation from corresponding R.sub.1, R.sub.2, R.sub.3 and R.sub.4 -substituted tetrahydroisoquinolines.

Abstract: Novel 7-ether and 7-thioether derivatives of 2-aryl, 3-aryl, and 2,3-diaryl-2,5,6,7-tetrahydro-3H-pyrrolo[1,2-a]-imidazole and 8-ether and 8-thioether derivatives of 2-aryl, 3-aryl, and 2,3-diaryl-2,3,5,6,7,8-hexahydro-imidazo[1,2-a]-pyridine, such as 2,3,5,6,7,8-hexahydro-2-phenyl-8,8-dimethoxy-imidazo[1,2-a]pyridine hydrochloride, useful as immunomodulators. Diether derivatives are prepared by reacting the corresponding monothioether derivative with a positive halogenating agent in the presence of an alcohol.

Abstract: The 2-aryl-1-aminoalkylcyclohexane nitrile, carboxylic acid or amide and derivatives thereof and methods of preparing same.

Abstract: The instantly claimed invention is a process for preparing a 3-aryl or a 2,3-diaryl-2,5,6,7-tetrahydro-3H-pyrrole[1,2-a]imidazole or a 3-aryl or a 2,3-diaryl-2,3,5,6,7,8-hexa-hydroimidazo[1,2-a]pyridine which comprises (a) contacting the acid addition salt of the corresponding cyclic methylthioimine with a 2-aryl or a 2,3-diarylaziridine and (b) recovering from the resultant reaction mixture the desired compound, useful as immunomodulators.

Abstract: The instantly claimed invention is a process for preparing novel 7-thioether derivatives of 2-aryl, 3 aryl, and 2,3-diary-2,5,7,7-tetra-hydro-3H-pyrrolo [1,2-a] imidazole and 8-thio-ether derivatives of 2-aryl, 3-aryl, and 2,3-diaryl-2,3,5,7,7,8-hexahydro-imidazo [1,2-a]-pyridine which comprises (a) contacting the corresponding amidine with about one molar equivalent of R.sub.1 SSR.sub.1 in the presence of about two molar equivalents of base and at a temperature of -78.degree. C. to about 0.degree. C. (b) contacting the corresponding amidine compound with about two molar equivalents of R,SSR, in the presence of about two molar equivalents of a base and at a temperature of from about -78.degree. C. to about 23.degree. C., said compounds being useful as immunomodulators.

Abstract: Novel 7-ether and 7-thioether derivatives of 2-aryl, 3-aryl, and 2,3-diaryl-2,5,6,7-tetrahydro-3H-pyrrolo[1,2-a]-imidazole and 8-ether and 8-thioether derivatives of 2-aryl, 3-aryl, and 2,3-diaryl-2,3,5,6,7,8-hexahydro-imidazo[1,2-a]-pyridine, such as 2,3,5,6,7,8-hexahydro-2-phenyl-8,8-dimethoxy-imidazo[1,2-a]pyridine hydrochloride, useful as immunomodulators.

Abstract: Certain 1,2,4,5-tetrahydro-7-alkoxy-(and 7,8-dialkoxy)-3H,3-benzazepines are prepared in excellent yields by a three step process comprising reacting a 3-alkoxy-(or 3,4-dialkoxy)-phenethylamine with a halo-acetaldehyde dialkylacetal to form the corresponding N-(2,2-dialkoxyethyl) phenethylamine, reacting that product with BF.sub.3 to close the ring and to form a 1-alkoxy-1,2,3,4-tetrahydro-7-alkoxy-(or 7,8-dialkoxy)-3H,3-benzazepine and reacting that product under reductive cleavage conditions to remove the 1-alkoxy group and to obtain the desired benzazepine. The benzazepines can be further reacted in the known manner or in the manner disclosed herein to form certain 3-substituted benzazepines.