专利号:US-10392364-B2 优先权日:2014-08-11 标题:Process for synthesis of lenalidomide 发明人:RAO RAMAKRISHNA; NANDIPATI RAMADEVI; GOODA RAVI; SHEWALKAR MUKESH PADMAKAR; BHADKE VENKAT VASANTRAO 权利人:AVRA LABORATORIES PVT LTD 摘要:Disclosed herein is an improved process for preparation of Lenalidomide and crystalline polymorphic forms thereof.
专利号:WO-2022222272-A1 优先权日:2021-04-19 标 题 :Synthesis process of 2-methyl-3-methoxybenzoic acid 发明人:GENG JINGKUN; Fang Zheneng; YAO LINXI; JI PINJUN; ZHANG YANCHAO; MIAO JUNHUI; WANG BOTAO 权利人:JIANGSU YONGAN CHEMICAL CO LTD 摘要:Disclosed is a synthesis process of 2-methyl-3-methoxybenzoic acid. The synthesis process comprises the following steps: (1) a reductive hydrogenation reaction, involving: using 2-methyl-3-nitrobenzoic acid or methyl 2-methyl-3-nitrobenzoate as a raw material, methanol as a solvent, hydrogen as a hydrogen source and palladium on carbon or platinum on carbon as a catalyst to prepare 3-amino-2-methylbenzoic acid or methyl 3-amino-2-methylbenzoate by means of hydrogenation reduction; (2) a one-pot reaction of diazotization, hydrolysis and esterification, involving: using the reduction product as a raw material and methanol as a solvent to prepare methyl 3-hydroxy-2-methylbenzoate by means of diazotization, hydrolysis and esterification reactions under the action of a diazotization reagent; (3) a methylation reaction, involving: using methyl 3-hydroxy-2-methylbenzoate as a raw material and dimethyl sulfate as a methylation reagent to prepare methyl 3-methoxy-2-methylbenzoate by means of a methylation reaction in the presence of an alkali; and (4) a hydrolysis reaction, involving: mixing methyl 3-methoxy-2-methylbenzoate with an alkali and water, and heating same for hydrolysis, cooling same after the reaction is completed, adjusting the pH to 1-3 with an acid to precipitate a product, followed by filtering and drying same to obtain 3-methoxy-2-methylbenzoic acid.
专利号:US-2018334443-A1 优先权日:2014-08-11 标题:An improved process for synthesis of lenalidomide
专利号:US-9522899-B2 优先权日:2009-06-01 标 题:Methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2, 6-dioxopiperidine, and intermediates thereof 发明人:YAN RONG; YANG HAO; XU YONGXIANG 权利人:NANJING CAVENDISH BIO-ENGINEERING TECH CO LTD; YAN RONG; NANJIAN CAVENDISH BIO-ENGINEERING TECH CO LTD 摘要:The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production.
专利号:WO-2016024286-A2 优先权日:2014-08-11 标 题 :An improved process for synthesis of lenalidomide
专利号:US-2003139451-A1 优先权日:2001-08-06 标题 :Synthesis and anti-tumor activity of nitrogen substituted thalidomide analogs
[参考文献]: M C Mcdonald, Et Al. Effects Of 5-Aminoisoquinolinone, A Water-Soluble, Potent Inhibitor Of The Activity Of Poly (Adp-Ribose) Polymerase On The Organ Injury And Dysfunction Caused By Haemorrhagic Shock. Br J Pharmacol. 2000 Jun;130(4):843-50.
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 108.