ChemInform Abstract: INTRAMOLECULAR CYCLIZATION OF ARYLALKYL ISOTHIOCYANATES. I. SYNTHESIS OF 1‐SUBSTITUTED 3,4‐DIHYDROISOQUINOLINES

Abstract

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 role of 5-arylalkylamino- and 5-piperazino- moieties on the 7-aminopyrazolo[4,3-d]pyrimidine core in affecting adenosine A1 and A2A receptor affinity and selectivity profiles

“…The commercially available phenyl-, 4-methoxyphenyl-, 2,4-dichlorophenyl- and benzyl-isothiocyanates or the suitably synthesized phenethyl- 29 , 4-methoxyphenethyl- 31 , 3,4-dimethoxyphenethyl- 30 , phenylpropyl-isothiocyanates 29 (1.97 mmol) were added to a solution of the 1-substituted-4-amino-pyrazole-3-carbonitriles 29–31 26 (1.64 mmol) in anhydrous DMF (1.5 mL). The mixture was stirred at room temperature for 3–4 h (compounds 32 – 34 , 38 , 39 ), for 16 h (compounds 35 , 40 , 42 ) and for 24 h (compounds 36 , 37 , 41 ).…”

“…Phenyl-, 4-methoxyphenyl-, 2,4-dichlorophenyl- and benzyl-isothiocyanates were commercially available, the others were synthesized as previously reported, i.e. allowing the corresponding arylalkylamines to react with CS 2 , in 30% hydrogen peroxide aqueous solution (phenylethyl-, phenylpropyl- and 3,4-dimethoxyphenyl-isothiocyanates) 29 , 30 or with thiophosgene and potassium carbonate, in CH 2 Cl 2 under nitrogen atmosphere (4-methoxyphenylisothiocyanate) 31 .…”