No abstract

The synthesis and biological properties of 35 2-(acylamino)oxazoles are described. The majority of the compounds inhibit the release of slow-reacting substance of anaphylaxis (SRS-A) in vitro from sensitized guinea pig chopped lung. In addition, several of the compounds inhibited the release of SRS-A from passively sensitized human chopped lung and protected guinea pigs from the effects of anaphylaxis in a modified Herxheimer test.

With triethyloxonium tetrafluoroborate or ethyl or methyl fluorosulphonate, 2-arylethyl isothiocyanates cyclised to give a 1 -ethylthio-or 1 -methylthio-3,4-dihydroisoquinoline, respectively. These compounds were prepared also by successive cyclisation of the isothiocyanates with aluminium chloride or polyphosphoric acid and alkylation of the resultant 3,4-dihydroisoquinoline-? (2H) -thione. They are useful starting materials for the synthesis of other 1 -substituted 3,4-dihydroisoquinolines, e.g. 1 -amino-compounds.?At approximately the time our first patent application 2 was published another appeared in which compounds (12), ( 14), and the hydroiodide of compound (1 7) are described along with several l-amino-3,4-dihydroisoquinolines [C.

Bei der Umsetzung des Isocyanats (I) mit Methyl‐fluorsulfonat bzw. Triäthyloxonium‐tetrafluoroborat entstehen direkt die entsprechenden Isochinoliniumsalze (II), aus denen die freien Basen (III) gewonnen werden.

The synthesis of variously substituted pyridazines by 1,4‐cycloaddition of cyclic enol ethers, esters, and some electron‐rich acetylenes is described. Extension of the scheme to include some imino‐ethers as dienophiles resulted in the synthesis of 1,2,4‐triazine derivatives.