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Reference
- 1-Piperazinecarboxamide derivatives
- 1-Piperazinecarboxamide derivatives. Bjoerk, Anders Karl Konrad; Fex, Tomas; Olsson, Knut Gunnar; Abramo, Aina Lisbeth; Gustafsson, Bengt Kenneth Roland; Christensson, Erik Gunnar (Aktieselskabet Ferrosan, Swed.). PCT Int. Appl. WO 8500811 A1 28 Feb 1985, 46 pp. DESIGNATED STATES: W: AU, DK, FI, HU, JP, NO, US. (English). (World Intellectual Property Organization). 97480-59-6 is the cas registry number. This chemical is also mentioned in this article. CODEN: PIXXD2. CLASS: ICM: C07D295-18. ICS: A61K031-495. APPLICATION: WO 84-SE269 2 Aug 1984. PRIORITY: SE 83-4361 10 Aug 1983. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 63 Title compds. I (R = H, halogen, CF3; R1, R2 = H, alkyl; R3, R4 = H, alkyl, alkenyl, cycloalkyl, aryl, aralkyl; NR3R4 = 5-7-membered satd. ring optionally contg. O, NR5, NCOR5; R5 = alkyl, alkenyl; X = CO, CHOH, CHOR6, CHO2R6, CH2, C:CR7R8, CHCHR7R8, 1,3-dioxolan-2-ylidene; R6 = alkyl, alkenyl; R7, R8 = H, alkyl; Z = O, S) were prepd. Thus, 4.0 g (0.017 mol) 1-[4-(4-fluorophenyl)butyl]piperazine in 20 mL PhMe was added to 0.97 g (0.017 mol) MeNCO in 35 mL PhMe at 5° and the whole stirred at 30-40° for 2 h to give piperazinecarboxamide II (R9 = Me), which was converted to 4.0 g monohydrochloride. II (R9 = Et) inhibited isolation-induced aggressive behavior in mice with ED50 3.5 mg/kg, s.c., compared with 6.7 mg/kg for Diazepam and blocked AcOH-induced writhing in mice with ED50 3.7 mg/kg, s.c. compared with 1.6 mg/kg for morphine. .


