CAS: 1050477-31-0; (S)-4-(4-Cyano-2-Methoxyphenyl)-5-Ethoxy-2,8-Dimethyl-1,4-Dihydro-1,6-Naphthyridine-3-Carboxamide

上下游产品

4-(4-Cyano-2-Methoxyphenyl)-5-Ethoxy-2,8-Dimethyl-1,4-Dihydro-1,6-Naphthyridine-3-Carboxamide 1050477-27-4
(4R)-4-(4-Cyano-2-Methoxyphenyl)-5-Ethoxy-2,8-Dimethyl-1,4-Dihydro-1,6-Naphthyridine-3-Carboxamide 1050477-30-9
4-(4-Cyano-2-Methoxyphenyl)-5-Ethoxy-2,8-Dimethyl-1,4-Dihydro-1,6-Naphthyridine-3-Carboxylic Acid 1050477-45-6
2-Cyanoethyl 4-(4-Cyano-2-Methoxyphenyl)-5-Ethoxy-2,8-Dimethyl-1,4-Dihydro-1,6-Naphthyridine-3-Carboxylate 1050477-44-5
2-Cyanoethyl 4-(4-Cyano-2-Methoxyphenyl)-2,8-Dimethyl-5-Oxo-1,4,5,6-Tetrahydro-1,6-Naphthyridine-3-Carboxylate 1050477-43-4

在 Sodium Phosphate体系中,用 乙醇,水 用作溶剂,20.0~38.0 °C,8.5 Kpa 条件下,反应 6.0H,以97.35%的收率获得
参考文献:Method For The Preparation Of (4S)-4-(4-Cyano-2-Methoxyphenyl)-5-Ethoxy-2,8-Dimethyl-1,4-Dihydro-1-6-Naphthyridine-3-Carbox-Amide By Racemate Separation By Means Of Diastereomeric Tartaric Acid Esters
标题:Method For The Preparation Of (4S)-4-(4-Cyano-2-Methoxyphenyl)-5-Ethoxy-2,8-Dimethyl-1,4-Dihydro-1-6-Naphthyridine-3-Carbox-Amide By Racemate Separation By Means Of Diastereomeric Tartaric Acid Esters
摘要:本发明涉及一种用于制备(4S)-4-(4-氰基-2-甲氧基苯基)-5-乙氧基-2,8-二甲基-1,4-二氢-1,6-萘啶-3-羧酰胺(i)的新型改进工艺,以及使用手性取代酒石酸酯(iiia)和(iiib)的一般式来进行外消旋分离制备对映体(ia),其中ar代表取代或未取代的芳香或杂芳基.

专利信息

专利号:US-12358877-B2
优先权日:2019-03-05
标题:Synthesis of 4-amino-5-methyl-1H-pyridin-2(1H)-on (intermediate compound for the synthesis of the MR antagonist finerenone) from 2-chloro-5-methyl-4-nitro-pyridine-1-oxide using the intermediate compound 2-chloro-5-methyl-4-pyridinamine
发明人：PLATZEK JOHANNES; LOVIS KAI
权利人:BAYER AG; Bayer Pharma AG
摘要:The present invention relates to a novel and improved method for preparing 4-amino-5-methylpyridone of the formula (I)which is an intermediate in the preparation of the MR antagonist finerenone.

专利号:WO-2023109968-A3
优先权日:2021-12-18
标 题:Synthesis method for finerenone and intermediate thereof
发明人：RUAN SHIWEN; ZHANG WEI; YAN GONGCHAO; ZHANG XINXIN
权利人:SHANGHAI DINGYA PHARMACEUTICAL CHEMICALS CO LTD
摘要:The invention provides a new synthesis method for a finerenone intermediate. The method comprises: (1) in the presence of an acid and in an inert solvent or under solvent-free conditions, reacting diethyl malonate, 4-cyano-2-methoxybenzaldehyde and 4-amino-5-methyl-2-hydroxypyridine to prepare compound 1; (2) subjecting compound 1 obtained in step (1) and triethyl orthoformate to an alkylation reaction in an inert solvent or under solvent-free conditions under the catalysis of an acid to obtain compound 2; (3) reducing compound 2 obtained in step (2) by using a reducing agent to obtain compound 3; and (4) in the presence of a catalyst, subjecting compound 3 and alcohol to chemical resolution to prepare chiral compound 4. The reaction formula is shown as follows: . By means of the technical solution of the present invention, the use of a chiral column resolution method is avoided, so that the cost is reduced; and by means of the chemical resolution, the loss of raw materials is reduced, the post-treatment is simple, and industrial large-scale production is facilitated.

专利号:EP-3935045-B1
优先权日:2019-03-05
标题 :Synthesis of 4-amino-5-methyl-1h-pyridin-2(1h)-one (intermediate in the synthesis of the mr antagonist finerenone) from 2-chloro-5-methyl-4-pyridinamine via the intermediate 2-chloro-5-methyl-4-pyridineamine

专利号:CO-2021011553-A2
优先权日:2019-03-05
标 题:Synthesis of 4-amino-5-methyl-1h-pyridin-2 (1h) -on (intermediate compound for the synthesis of the antagonist mr finerenone) from 2-chloro-5-methyl-4-nitro-pyridine-1 -oxide using the intermediate 2-chloro-5-methyl-4-pyridinamine

专利号:MX-2021010612-A
优先权日:2019-03-05
标题 :Synthesis of 4-amino-5-methyl-1h-pyridin-2(1h)-on (intermediate compound for the synthesis of the mr antagonist finerenone) from 2-chloro-5-methyl-4-nitro-pyridine-1-oxide using the intermediate compound 2-chloro-5-methyl-4-pyridinamine.

专利号:CL-2021002316-A1
优先权日:2019-03-05
标题:Synthesis of 4-amino-5-methyl-1h-pyridin-2(1h)-on (intermediate compound for the synthesis of the antagonist mr finerenone) from 2-chloro-5-methyl-4-nitro-pyridine-1- oxide using the intermediate compound 2-chloro-5-methyl-4-pyridinamine