Reference

2-[4-(2-Furoyl)-1-piperazin-1-yl]-4-amino-6,7-dimethylquinazoline-contai ning antihypertension drugs

2-[4-(2-Furoyl)-1-piperazin-1-yl]-4-amino-6,7-dimethylquinazoline-contai ning antihypertension drugs. Winn, Martin; Kyncl, Jaroslav; Dunnigan, Daniel Ambrose; Jones, Peter Hadley (Abbott Laboratories, USA). Ger. Offen. DE 2646186 28 Apr 1977, 22 pp. (German). (Germany). CODEN: GWXXBX. CLASS: IC: C07D405-14. PRIORITY: US 75-621980 14 Oct 1975. DOCUMENT TYPE: Patent CA Section: 1 (Pharmacodynamics) Section cross-reference(s): 28 2-[4-(2-Furoyl)-1-piperazinyl]-4-amino-6,7-dimethylquinazoline derivs. with good H2O soly. are prepd. and show antihypertensive activity. For example, 39 g N-(2-furoyl)piperazine-HBr [63074-06-6] was hydrogenated and then treated with NaOH to give 22.5 g N-(tetrahydro-2-furoyl)piperazine [63074-07-7]. This compd. (10.8 g) was refluxed with 7 g 2-chloro-4-amino-6,7-dimethoxyquinazoline [23680-84-4] to give 8.12 g 2-[4-(tetrahydro-2-furoyl)-1-piperazinyl]-4-amino-6,7-dimethoxyquinazoli ne-HCl (I) [63074-08-8]. I had water soly. of 590 mg/mL.Several reagents such as 63074-09-9 is used here. An i.p. dose of 30 mg I/kg decreased the blood pressure 20-60% for >24 h in spontaneous hypertonic rats. A 3-10 mg/kg oral dose gave a .ltoreq.40% decreaase. .