Patent classifications
C07C227/12
Full continuous-flow preparation method of L-carnitine
A full continuous-flow preparation method of L-carnitine, including: mixing chlorine gas and a diketene solution via a first micromixer followed by transportation to a first microchannel reactor for continuous chlorination and esterification reaction to obtain 4-chloroacetoacetate; feeding the 4-chloroacetoacetate and a reductase to a second micromixer and a second microchannel reactor in sequence for continuous catalytic reaction to obtain (R)-4-chloro-3-hydroxybutyrate; simultaneously transporting the (R)-4-chloro-3-hydroxybutyrate and a trimethylamine solution to a third micromixer and a third microchannel reactor for continuous substitution and hydrolysis reaction; and subjecting the reaction mixture to desalination and concentration to obtain the L-carnitine.
FULL CONTINUOUS-FLOW PREPARATION METHOD OF L-CARNITINE
A full continuous-flow preparation method of L-carnitine, including: mixing chlorine gas and a diketene solution via a first micromixer followed by transportation to a first microchannel reactor for continuous chlorination and esterification reaction to obtain 4-chloroacetoacetate; feeding the 4-chloroacetoacetate and a reductase to a second micromixer and a second microchannel reactor in sequence for continuous catalytic reaction to obtain (R)-4-chloro-3-hydroxybutyrate; simultaneously transporting the (R)-4-chloro-3-hydroxybutyrate and a trimethylamine solution to a third micromixer and a third microchannel reactor for continuous substitution and hydrolysis reaction; and subjecting the reaction mixture to desalination and concentration to obtain the L-carnitine.
FULL CONTINUOUS-FLOW PREPARATION METHOD OF L-CARNITINE
A full continuous-flow preparation method of L-carnitine, including: mixing chlorine gas and a diketene solution via a first micromixer followed by transportation to a first microchannel reactor for continuous chlorination and esterification reaction to obtain 4-chloroacetoacetate; feeding the 4-chloroacetoacetate and a reductase to a second micromixer and a second microchannel reactor in sequence for continuous catalytic reaction to obtain (R)-4-chloro-3-hydroxybutyrate; simultaneously transporting the (R)-4-chloro-3-hydroxybutyrate and a trimethylamine solution to a third micromixer and a third microchannel reactor for continuous substitution and hydrolysis reaction; and subjecting the reaction mixture to desalination and concentration to obtain the L-carnitine.
Building blocks for stapled peptides
This invention relates to a method for producing an alkenyl 1-aminocyclopropane-1-carboxylic acid of Formula I wherein R.sup.1 is a protecting group, n is an integer between 1 and 10, and A and B are chiral centres such that when A is S, B is R and when A is R, B is S. The method comprises a stereoselective formation of the cyclopropane moiety by cycloaddition onto a double bond, in a molecule comprising a chiral template, Formula lc. Further provided is the use of Formula I in the production of stapled peptides. ##STR00001##
Building blocks for stapled peptides
This invention relates to a method for producing an alkenyl 1-aminocyclopropane-1-carboxylic acid of Formula I wherein R.sup.1 is a protecting group, n is an integer between 1 and 10, and A and B are chiral centres such that when A is S, B is R and when A is R, B is S. The method comprises a stereoselective formation of the cyclopropane moiety by cycloaddition onto a double bond, in a molecule comprising a chiral template, Formula lc. Further provided is the use of Formula I in the production of stapled peptides. ##STR00001##
Pharmaceutically Active Compounds
The invention is directed to compounds of general formula (I)
##STR00001##
and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.
Pharmaceutically Active Compounds
The invention is directed to compounds of general formula (I)
##STR00001##
and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.
Pharmaceutically Active Compounds
The invention is directed to compounds of general formula (I)
##STR00001##
and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.
Process for the preparation of a chelating agent
It is provided a compound of formula (I); wherein R.sup.5 is selected from the group consisting of H, OM, COOM, NH.sub.2, SO.sub.3M, (C.sub.1-C.sub.4)alkyl, and halogen; and A is a radical having at least 3 C atoms selected from the group consisting of: i) a radical of formula (i) wherein R.sup.7 is selected from the group consisting of OM, and COOM, and n is 0, 1 or 2; and ii) a radical of formula (ii) or of formula (iii) wherein R.sup.8 is selected from the group consisting of H, (C.sub.1-C.sub.4)alkyl; and wherein M is independently selected from the group consisting of H, an alkaly metal, and NH.sub.4.sup.+. It is also provided a process for the preparation thereof, a composition comprising it, and its use for correcting deficiencies of metals in plants. ##STR00001##
Process for the preparation of a chelating agent
It is provided a compound of formula (I); wherein R.sup.5 is selected from the group consisting of H, OM, COOM, NH.sub.2, SO.sub.3M, (C.sub.1-C.sub.4)alkyl, and halogen; and A is a radical having at least 3 C atoms selected from the group consisting of: i) a radical of formula (i) wherein R.sup.7 is selected from the group consisting of OM, and COOM, and n is 0, 1 or 2; and ii) a radical of formula (ii) or of formula (iii) wherein R.sup.8 is selected from the group consisting of H, (C.sub.1-C.sub.4)alkyl; and wherein M is independently selected from the group consisting of H, an alkaly metal, and NH.sub.4.sup.+. It is also provided a process for the preparation thereof, a composition comprising it, and its use for correcting deficiencies of metals in plants. ##STR00001##