摘要 |
Title compds.≮I; R = Me, Et, Pr; R1 = C1-2 alkoxycarbonyl, CONHCHR2CH2OH(R2 = Me, Et,), CH2R3(R3 = MeS, MeSO2, MeO, Cl, Br, HO, CN, C1-3 alkylsulfonyloxy, p-MeC6H4SO3, PhSO3); dashes represents single or double bond≉ were prepd. Thus, D-6-n propyl-8β-(methoxymethyl) ergoline methanesulfonate was cleaved with sodium periodate followed by hydrolysis to give 2-(methoxymethyl)-4-propyl-6- oxo-7- amino-1,2a,3,4,4a,5,6,10ba-octahydrobenzo≮f≉quinoline, which underwent diazotization-cyclization to give D-6-n-propyl-8-(methoxymethyl)-2-azaergoline. At 3 mg/kg D-6-methyl-8-(methylthiomethyl)-aza ergoline was a neuroleptic.
|