CAS: 253168-94-4; 1-(3-Ethoxy-4-Methoxyphenyl)-2-(Methylsulfonyl)Ethanamine

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CAS号608141-42-0 (S)-1-(3-乙氧基-4-...

3-羟基-4-甲氧基苯甲酸甲酯置于potassium Tert-Butylate,甲酸铵,Potassium Carbonate体系中,用 甲醇,水,二甲基亚砜,丙酮 用作溶剂,化学反应 28.0H,反应生成阿普斯特中间体
参考文献:一种合成1-(3-乙氧基-4-甲氧基)苯基-2-甲磺酰基乙胺的方法
标题:一种合成1-(3-乙氧基-4-甲氧基)苯基-2-甲磺酰基乙胺的方法
摘要:本发明公开了一种合成1‑(3‑乙氧基‑4‑甲氧基)苯基‑2‑甲磺酰基乙胺的方法,属于有机合成工艺技术领域.该方法是以3‑羟基‑4‑甲氧基苯甲酸为原料,先经酯化反应得3‑羟基‑4‑甲氧基苯甲酸甲酯,再与溴乙烷反应得3‑乙氧基‑4‑甲氧基苯甲酸甲酯,后与二甲基砜反应得1‑(3‑乙氧基‑4‑甲氧基)苯基‑2‑甲磺酰基乙酮,最后与甲酸铵发生还原胺化反应制得1‑(3‑乙氧基‑4‑甲氧基)苯基‑2‑甲磺酰基乙胺.

专利信息

专利号:WO-2016192694-A1
优先权日:2015-06-05
标 题 :A process for preparing the key intermediate of apremilast, using enzymatic resolution of the racemic amines
发明人：DOUBSKY JAN; KLVANA ROBERT; RICHTER JINDRICH; Lehnert Petr
权利人:ZENTIVA KS
摘要:The invention relates to a preparation method of (S)-l-(3-ethoxy-4-methoxyphenyl)- 2-(methylsulfonyl)-ethyl-amine (S)-l, or its N-acyl derivatives of general formula (S)-2. The amine (S)-l is the key intermediate in the synthesis of (S)-{2-[l-(3-ethoxy-4- methoxyphenyi)-2-methyisulfonylethyl]-4-acetylaminoisoindolin-l ?3-dione, known as Apremilast. In this synthesis, the amine (S)-l, or its respective salts, are subjected to condensation with 3-acetamidophthalic anhydride 4, providing the desired product 3 (Scheme 1).

专利号:US-8242310-B2
优先权日:2008-09-10
标题:Processes for the preparation of aminosulfone compounds
发明人：SAINDANE MANOHAR T; GE CHUANSHENG
权利人:SAINDANE MANOHAR T; GE CHUANSHENG; CELGENE CORP
摘要:Processes for synthesizing aminosulfone compounds are provided. Aminosulfone compounds obtained using methods provided herein are useful in production or synthesis of isoindoline based PDE 4 modulators.

专利号:US-9688623-B2
优先权日:2012-02-21
标题:Processes for the preparation of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethylamine
发明人：VENKATESWARALU JASTI; RAJENDIRAN CHINNAPILLAI; REDDY NALLAMADDI RAVIKUMAR; CONNOLLY TERRENCE JOSEPH; RUCHELMAN ALEXANDER L; ECKERT JEFFREY; FRANK ANTHONY JOSEPH
权利人:CELGENE CORP
摘要:Provided herein are new processes for the preparation of aminosulfone intermediates for the synthesis of 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, which is useful for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-α. Further provided herein are processes for the commercial production of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethylamine.

专利号:US-9126906-B2
优先权日:2012-02-21
标 题:Asymmetric synthetic processes for the preparation of aminosulfone compounds
发明人：CONNOLLY TERRENCE J; RUCHELMAN ALEXANDER L; LEONG WILLIAM W
权利人:CELGENE CORP
摘要:Processes for synthesizing aminosulfone compounds are provided. The processes provided herein utilize asymmetric reduction reactions, e.g., asymmetric hydrogenation, of protected or unprotected enamine or ketone substrates. Aminosulfone compounds obtained using methods provided herein are useful in production or synthesis of sulfone group containing isoindoline based compounds.

专利号:EP-3280701-B1
优先权日:2015-04-09
标 题 :A method of chiral resolution of the key intermediate of the synthesis of apremilast and its use for the preparation of pure apremilast
发明人：FAIGL FERENC; DOUBSKY JAN; KLVANA ROBERT; RICHTER JINDRICH; FOGASSY ELEMER; MATRAVOLGYI BELA; MIZSAK AGNES
权利人:ZENTIVA KS

专利号:CN-110467557-B
优先权日:2018-05-11
标题 :Three-component one-pot boiling synthesis method of apremilast