Synthesis of active compounds of different Jacquelina
Abstract
Benzylispquinolines of pharmacological activity, most of the role of the sympathetic nerve. The laboratory has found that a cardiac
The role of birds to a test, itscatechol structure on the base, through modification into Coclaurine or Isococlaurine
Later, its role in a container by the sympathetic nervous stimulants by B antagonist into the trend. Also according to Isopro
terenol and Trimethoquinolthe catecholstructure, was modified into a dichloro- substituted derivatives, the effect
Confirmed by the container into the sympathetic beta-blocker phenomenon. If
the birds in to a base structure on the catecholdrugs
Base to make the appropriate modifications, is likely to be a potential sympathetic beta-blocker by the container.
Using chemical synthesis methods, preparation of the derivatives of four different .
(1) by Bischler- Napieralski cyclization synthesis of 41,42 and 43: respectively piperona
l (15), vanillin (14), and 2 - naphthaldehyde (17) such as the starting material, by
After a β-nitrovinyl derivatives, arylethylamines, andamides and other intermediate products, then further
Step by Bischler- Napieralski cyclization, and reduction, remove the protecting group and a few steps of the reaction, the last available
Were obtained (±) - Norcinnamolaurine (41 ),(±) N - Norarmepavine (42)
, And 1 - (4'-hydroxybenzyl) -1,2,3,4 - tetrahydrobenzo〕 〔h isoquinoline (43) and other compounds.
(2) was synthesized by Reissert 58: The 3,4 - dichlorobenzaldehyde (45) as the starting
Material, by Pomeranz - Fritsch reaction available simpleisoquinoline, via Reissert compounds
As well as hydrolysis, hydrogenation, the reaction to remove protecting groups, etc., the last available one-dichloro-substituted benzylisoquinoli
ne derivatives 58.
Synthesis of compounds 41,42 and 43 throughout the total yield was 17.3%, 13.0%, and 18
. 0% Preparation of compound 58, the total yield of 6.5%.
These four compounds in the sympathetic role of B by blocking the activity of the container, will be from animal tissue
To assessment.
English Abstract
