CAS: 6118-65-6; N-(1,3-Dioxoisoindolin-4-yl)Acetamide

上下游产品

3-aminophthalimide acetic anhydride 3-nitrophthalic acid anhydride 4-nitro-1H-isoindole-1,3(2H)-dione 6-acetylamino-anthranilic acid 3-acetylaminophthalic acid Apremilast R-Apremilast

📜3-硝基邻苯二甲酸酐置于ammonium Hydroxide,10% Pt/activated Carbon,氢气体系中,用 乙醇 作为反应溶剂,80.0~230.0 °C,202.66 Kpa 条件下,反应 27.0H,反应生成 3-乙酰氨基邻苯二甲酰亚胺
参考文献:Chemoenzymatic Synthesis Of Apremilast: A Study Using Ketoreductases And Lipases
标题:Chemoenzymatic Synthesis Of Apremilast: A Study Using Ketoreductases And Lipases
摘要:在阿普雷米拉斯的化学酶合成中的关键步骤是产生手性醇(R)-1-(3-乙氧基-4-甲氧基苯基)-2-(甲磺基)乙醇,(R)-3.评估了两种酶法来获得(R)-3,一种使用酮还原酶,另一种使用脂肪酶.使用酮还原酶kred-P2-D12对1-(3-乙氧基-4-甲氧基苯基)-2-(甲磺基)乙酮(2)进行生物还原,导致(R)-3,转化率为48%,对映体过量为93% (Ee).通过利用黑曲霉脂肪酶催化,对手性纯(R)-3和4-乙酰氨基异吲哚-1,3-二酮(8)之间的反应,得到了65%的产率和67%的ee的阿普雷米拉斯.
DOI:10.21577/0103-5053.20210012

专利信息

专利号:WO-2016202806-A1
优先权日:2015-06-15
标题:A novel synthetic pathway towards apremilast
发明人：STAVBER GAJ
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to a process for providing a chiral β-hydroxysulfone compound, an intermediate useful in the synthesis of the isoindoline-based compound apremilast.

专利号:CN-108084078-B
优先权日:2016-11-24
标题 :Synthesis method of medicine apremilast for treating psoriatic arthritis diseases