1050477-31-0Relevant articles and documents
Synthetic method of fenerenone and intermediate thereof
-
Paragraph 0037-0039, (2022/04/06)
The invention provides a novel synthetic method of a fenerenone intermediate. The method comprises the following steps: (1) in the presence of an acid and in an inert solvent or solvent-free condition, carrying out a reaction on diethyl malonate, 4-cyano-2-methoxybenzaldehyde and 4-amino-5-methyl-2-hydroxypyridine to prepare a compound 1; (2) carrying out alkylation reaction on the compound 1 obtained in the step (1) and triethyl orthoformate in an inert solvent or solvent-free condition under acid catalysis to obtain a compound 2; (3) reducing the compound 2 obtained in the step (2) through a reducing agent to obtain a compound 3; (4) in the presence of a catalyst, splitting the compound 3 and alcohol by a chemical method to prepare a chiral compound 4; the reaction formula is shown in the specification. By applying the technical scheme provided by the invention, a chiral column splitting method is avoided, so that the cost is reduced; by adopting a chemical method for splitting, the raw material loss is reduced, the post-treatment is simple, and the industrial large-scale production is facilitated.
PROCESS FOR PREPARING (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE-3-CARBOXAMIDE ENABLED BY A CATALYTIC ASYMMETRIC HANTZSCH ESTER REDUCTION
-
, (2022/01/06)
The present invention relates to a novel process for preparing (4S)-4-(4-Cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide by an asymmetric Hantzsch ester reduction of racemic 4-(4-Cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,6-naphthyridine-3-carboxamide.
METHOD FOR THE PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOXAMIDE AND RECOVERY OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOXAMIDE BY ELECTROCHEMICAL METHODS
-
Paragraph 0217-0229, (2018/09/16)
The present invention relates to a novel process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and recovering (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) proceeding from (4R)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula ent-(I)