Title:
MANUFACTURE OF NOVEL PYRIMIDINE COMPOUND
Document Type and Number:
Japanese Patent JPS5823666
Kind Code:
A
Abstract:
Title cpds. of formula (I) and their condensation prod. with aldehydes, ketones and carbonic acid, and N-oxides are new: Het.O.CH2.CH(OH).CH2.NHC(CH3)R1R2 (I) (where Het = opt. substd. pyridazinyl, pyrimidinyl or pyrazinyl or substd. pyridyl; R = H or Me; R2 = lower alkyl opt. substd. by Ph (itself opt. substd.), CO2H or functionally modified CO2H). (I) where Het = substd. diazinyl are beta-adrenergic blockers (some cordioselective) and some also have intrinsic sympathomimetic activity; the unsubtd. pyrazines and pyrimidines stimulate the beta-receptors with positive inotropic and chromotropic actions; they are thus useful in treating various cardiac and circulatory disorders. Suitable methods of preparation include (a) reaction of Het.O.CH2.CH(X').CH2.Z' and Z2.C(CH3)R1R2 (one of Z' and Z2 = NH2 other is reactively esterified OH and X' = OH; or Z' + X' = epoxy and Z2 = NH2); (b) reaction of Het Z and HO.CH2.CH(OH)CH2.NH.C(CH3)R1R2 (Z = nucleophilically displaceable gp.); opt. the diol is replaced by its condensation prod. with carbonyl cpds.; (c) removal of protecting gps. from OH and/or NH2; (d) reduction of corresp. Schiff's base. Many cpds. are specifically claimed e.g. 5-Br-3-morpholino-2-(3-isopropylamino-2-hydroxypropoxy)pyrazine hydrochloride.
Inventors:
IERUKU FURAI
KUNUTSUTO AA IETSUGI
FURANTSU OSUTERUMAIA
HERUBERUTO SHIYURETSUTA
KUNUTSUTO AA IETSUGI
FURANTSU OSUTERUMAIA
HERUBERUTO SHIYURETSUTA
Application Number:
JP13230182A
Publication Date:
February 12, 1983
Filing Date:
July 30, 1982
Export Citation:
Assignee:
CIBA GEIGY AG
International Classes:
C07D239/34; A61K31/4965; A61K31/497; A61K31/505; A61P25/02; C07C67/00; C07C213/00; C07D213/16; C07D213/61; C07D213/64; C07D213/69; C07D213/75; C07D213/78; C07D213/80; C07D213/82; C07D213/85; C07D213/89; C07D239/47; C07D239/52; C07D239/56; C07D241/18; C07D241/20; C07D263/06; C07D405/12; C07D413/12; C07D237/06; C07D239/24; C07D241/02; (IPC1-7): A61K31/44; A61K31/455; C07C91/10; C07D213/61; C07D213/64; C07D213/69; C07D213/73; C07D213/75; C07D213/78; C07D213/80; C07D213/82; C07D213/85; C07D213/89; C07D263/06; C07D405/12; C07D413/04
Attorney, Agent or Firm:
Nobuhiko Nakajima