| 摘要 |
<p>(A) prodn. of pyrido-benzodiazepines of formula (I), and their acid addn. salts except when R= alkali metal, comprises reacting a cpd. (II) with at least a stoichiometric amt. of strong, non-nucleophilic alkali metal base in an inert liq. carrier to give (I; R=Ra). This cpd. with R=alkali metal is opt. reacted with a proton source to give R=H, then opt. reacting this with halo-alk1-Q. - R = alkali metal cation, H or -alk1-Q; alk1 = 1-8C opt. branched hydrocarbyl; Q = H, halo, NR1R2, -N=CH.OEt or 2-tetrahydropyranyloxy; R1 and R2 = lower alkyl or lower alkoxycarbonyl, or together complete 1-piperidinyl, 1-phthalimido, 1-pyrrolidinyl, 4-morpholinyl or opt. 4-substd. piperazin-1-yl. Ar = 2-,3- or 4-pyridyl; 2- or 3-thienyl or phenyl (opt.substd. by 1-3 same or different halo, lower alkyl or alkoxy, CF3 or NO2); Z = H, halo, lower alkyl or alkoxy, OH or NO2; Y = H or 1 or 2, same or different, lower alkyl or alkoxy, or OH X = Cl,Br,F or I; Ra=R other than alkali metal or -alk1-halo. Alternatively, (II) is replaced by a mixt. of (III) and (IV). (B) Cpds.(II) and (III) are new cpds. where Ra=H, lower alkyl or -alk1-Q' (Q' = NR1R2, -N=CHOEt or 2-tetrahydropyranyloxy) in (II) or -alk1-Q' in (III).</p> |
