- STEREOCHEMICAL STUDIES, 145. SATURATED HETEROCYCLES, 152. PREPARATION AND CONFORMATIONAL ANALYSIS OF STEREOISOMERIC 1,6,7,11b-TETRAHYDRO-2HOXAZINOISOQUINOLIN-4-ONE DERIVATIVES
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Starting from 1--6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline 3a, trifunctional 1,2,3,4-tetrahydroisoquinolines were synthetized.From the N-ethoxycarbonyl derivative of 3a, (r-11b,c-1)-1-hydroxymethyl- (8) and (r-11b,t-1)-1-chloromethyl-9,10-dimethoxy-1,6,7,11b-tetrahydro-2Hoxazinoisoquinolin-4-one (9) were formed in unexpected reactions.High-resolution NMR revealed that the tetrahydroisoquinoline-fused C-1 epimer oxazinone derivatives 8 and 9 have different conformations in solution.The first X-ray diffraction evidence of the presence of two different conformations of oxazinoisoquinolines 8 and 9 in the solid state is provided.
- Lazar, Laszlo,Fueloep, Ferenc,Dombi, Gyoergy,Bernath, Gabor,Argay, Gyula,Kalman, Alajos
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p. 4039 - 4048
(2007/10/02)
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- 1-(hydroxymethyl)-1,6,7,11b-tetrahydro-2H,4H-[1,3]oxazino- or -thiazino-[4,3-a]isoquinoline derivatives and pharmaceutical compositions containing them
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The invention relates to 1-(hydroxymethyl)-1,6,7,11b-tetrahydro-2H,4H-[1,3]oxazino- or -thiazino-[4,3-a]isoquinoline derivatives of the formula (I), STR1 wherein R1 and R2 are alkoxy having from 1 to 6 carbon atoms, X is oxygen or su
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