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:US-8344118-B2 优先权日:2007-10-31 标 题 :Preparation and isolation of 5′ capped MRNA 发明人:KORE ANILKUMAR; MUTHIAN SHANMUGASUNDARAM; CHARLES IRUDAYA 权利人:APPLIED BIOSYSTEMS LLC; KORE ANILKUMAR; MUTHIAN SHANMUGASUNDARAM; CHARLES IRUDAYA 摘要:The synthesis of capped/tagged RNA, methods of use and kits providing same are contemplated. Tagged RNA permits isolation of RNA transcripts in vitro. The ability to isolate and purify capped RNA results in improved transcription and translation and provides a tool for identifying RNA-protein interactions. Such capped RNA finds use in therapeutic applications, diagnosis and prognosis and in the treatment of cancers and HIV.
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:WO-2020178175-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 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: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