Reference

Process for producing ethylenamines

Process for producing ethylenamines. Hara, Yasushi; Hironaka, Toshio; Nagasaki, Noritaka; Kanai, Nobuyuki; Suzuki, Nobumasa; Ito, Yukio; Miyake, Takanori (Tosoh Corp., Japan). Eur. Pat. Appl. EP 476578 A1 25 Mar 1992, 19 pp. DESIGNATED STATES: R: BE, DE, FR, GB, NL, SE. (European Patent Organization). CODEN: EPXXDW. CLASS: ICM: C07C209-16. ICS: C07D295-12; B01J023-76. APPLICATION: EP 91-115736 17 Sep 1991. PRIORITY: JP 90-243830 17 Sep 1990; JP 90-322352 28 Nov 1990; JP 90-415070 27 Dec 1990; JP 91-159435 4 Jun 1991; JP 91-159437 4 Jun 1991; JP 91-189572 4 Jul 1991. DOCUMENT TYPE: Patent CA Section: 23 (Aliphatic Compounds) The title compds. were prepd. by reaction of an ethanolamine with NH3 and/or an ethylenamine in the presence of H2 and a catalyst contg. Ni and a rare earth metal. Thus, HOCH2CH2NH2 (I) and NH3 reacted in the presence of a Ni-Y-silica gel catalyst at 200°/192 kg/cm2 for 3 h to give a product mixt. 140-31-8 and 103-76-4 are also in the experiment. with the following selectivities in mol %: ethylenediamine, 57.3; piperazine, 7.9; diethylenetriamine, 10.1; N-(2-aminoethyl)ethanolamine, 8.5; N-(2-aminoethyl)piperazine, 1.3; N-(2-hydroxyethyl)piperazine, 0.6. The conversion of I was 43.3%. .

Heterocyclic systems

Heterocyclic systems. IV. Synthesis and CNS activity of 4H,6H-pyrrolo[1,2-a][4,1]benzoxazepine derivatives. Massa, S.In this study， 88442-94-8 and 103-76-4 are also used.; Corelli, F.; Pantaleoni, G. C.; Palumbo, G. (Ist. Chim. Farm. Tossicol., Univ. "La Sapienza", Rome, Italy). Farmaco, Ed. Sci., 38(11), 893-903 (Italian) 1983. CODEN: FRPSAX. ISSN: 0430-0920. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 28 Ten title compds. (I; R = H or Cl; R1 = H, CHO, CH2OH, CH2OMe, CH:NNH2, CH2NMe2, or cyclic groups contg. N; R2 = H or Ph) were prepd. and tested in mice for activity on the CNS (central nervous system), measuring various parameters correlated with benzodiazepine receptor types I and II. The most active compd. was the unsubstituted 4H,6H-pyrrolo[1,2-a][4,1]benzoxazepine (I; R = R1 = R2 = H) [79100-18-8], which had sedative activity and protected against electroshock; its action thus seemed to involve both types of benzodiazepine receptors, but it was only ~10% as active as diazepam. Some structure-activity relations are discussed, and the prepn. of all I and some intermediates is described. .