- Convenient synthesis of tolcapone, a selective catechol-O-methyltransferase inhibitor
-
A convenient and efficient synthesis of tolcapone from commercial 4-benzyloxy-3-methoxybenzaldehyde is presented. Grignard reaction of 4-benzyloxy-3-methoxybenzaldehyde (1) with p-tolylmagnesium bromide followed by Oppenauer oxidation of the hydroxyl func
- Manikumar, Govindarajan,Jin, Chunyang,Rehder, Kenneth S.
-
p. 810 - 815
(2008/09/16)
-
- Process for the preparation of benzophenone derivatives
-
The present invention relates to a process for the preparation of benzophenone derivatives and comprises a selective crystallization of alkali salts of compounds of formula (I) STR1 wherein R1 is lower-alkyl and R2 is hydrogen, lower
- -
-
-
- Catechol derivatives
-
Catechol derivatives of the formula STR1 wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure. Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
- -
-
-
