摘要:
A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position.
摘要:
The invention relates to a new method for preparing (R)-praziquantel. In the invention, by taking advantage of the high stereo selectivity, site selectivity and region selectivity of an enzyme, an intermediate of a pure optical and chiral (R)-praziquantel are obtained by means of the dynamic kinetic resolution of an enantiomer from the synthesized racemate or derivatives thereof, and the (R)-praziquantel is obtained by using various conventional and mature organic chemical reactions with higher yield. The method of the invention has the potential advantages of easily available raw materials, low cost, environmentally safer process and convenience for large-scale production. Also, the purity of the end product can be more than 98%. By adopting the invention, the quality of the product is improved and a basis for developing high quality of active pharmaceutical ingredients and formulations is established, and thus the pending industrial problem of purifying praziquantel over 30 years becomes solvable.
摘要:
The present invention relates to a biocatalytic method of preparing a mono-acylated polyol catalyzed by triacylglycerol lipase mutants, as for example derived from Candida antarctica lipase B (CALB); a biocatalytic method of enantioselectively preparing an asymmetric mono-acylated polyol, catalyzed by the same enzyme mutants; as well as the use of a mutated triacylglycerol lipase in a method of preparing mono-acylated polyols. The invention also provides novel mutants, coding sequences thereof, and recombinant microorganisms carrying said coding sequences.
摘要:
The present invention provides novel processes of preparing racemic and optically active cyclopentenones of Formula I: The invention also provides novel cyclopentenones of formula I in racemic or optically active form.
摘要:
The present invention relates to the preparation of isomerically pure substituted cyclohexanols starting from a mixture of cis/trans substituted cyclohexanols which comprises reacting the cis/trans mixture of a substituted cyclohexanol with a dicarboxylic acid anhydride in the presence of a lipase, to give the trans semi-ester which is separated off from the unreacted substituted cyclohexanol cis isomer.
摘要:
A compound 4-((1R,3S)-6-Chloro-3-phenylindan-1-yl)-2,2-dimethylpiperazine and salts thereof, pharmaceutical compositions comprising the compound and salts, and medical use thereof, including for treatment of schizophrenia and other psychotic disorders.
摘要:
Disclosed is a method for producing chiral, secondary alcohols of formula (I), wherein A represents an aromatic, heterocyclic, or alicyclic ring or a ring system with 4 to 20 C atoms, n represents 0, 1, 2, 3, 4, or 5, R represents halogen, OH, an O— protective group, NO2, N,N—R2,R3 amine, R2 and R3 representing C1-C6 alkyl, phenyl, or benzyl, N,N—R2,R3-amino-C1-C6 alkyl, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C4 alkoxycarbonyl, or CN, and R1 represents N,N—R2,R3 amine, N,N—R2,R3-amino-C1-C6 alkyl, C1-C12 alkyl, C1-C6-haloalkyl, C1-C4 alkoxycarbonyl, C1-C6 alkoxy-C1-C6 alkyl, or a C2-C5 alkylene radical that forms a ring system along with the A radical. According to the inventive method, a) a ketone of formula (II) is optionally reduced to the corresponding racemic alcohol of formula (III) by means of an aliphatic C1-C6 alcohol in the presence of a transition metal catalyst and a base, and b) the alcohol of formula (III) is reacted to a mixture of (R) ester of formula (IV), wherein R4 represents H or C1-C5 alkyl, and (S) alcohol of formula (I) in the presence of an esterification catalyst and an acyl donor, whereupon the (S) alcohol is isolated from the reaction mixture by means of crystallization or distillation according to the aggregate state thereof.
摘要:
A method for increasing the rate of chemical reactions involving the conversion of at least one reactant to at least one product involves contacting the reactant with an appropriate monoclonal antibody under conditions permitting the formation of a complex between the antibody and the reactant. The complexed reactant is converted to the product which is then released from the complex. The monoclonal antibody may employ a cofactor and may be directed to a known substrate of an enzyme. Methods for preparing such monoclonal antibodies are also disclosed.
摘要:
A chiral compound, particularly a chiral secondary alcohol, can be efficiently resolved under a mild condition by acylation with an alkenyl acetate in the presence of a novel aminocyclopentadienyl ruthenium complex, an enzyme catalyst, and a base.